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Journal articles on the topic 'Piperazine Synthesis'

Author: Grafiati
Published: 11 December 2022
Last updated: 25 January 2023

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1

Kmoníček, Vojtěch, Martin Valchář, and Zdeněk Polívka. "Some 4-Substituted 1-(3-Pyridylmethyl)piperazines with Antihistamine Activity." Collection of Czechoslovak Chemical Communications 59, no. 10 (1994): 2343–50. http://dx.doi.org/10.1135/cccc19942343.

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Several compounds derived from nicotinic acid were prepared within a more extensive programme aiming at the synthesis of new substances with expected antihistamine and antidepressant activity. Some of these compounds display certain structural resemblance with the antidepressant agent piberaline (EGYT 475, Trelibet®, I) and its analogues. The products were used as intermediates for the synthesis of further compounds and most of them were subjected to pharmacological testing. Substituted nicotinic acid piperazides IIa - IId and IVa - IVe were obtained by reactions of nicotinoyl chloride (prepared in situ) with the correspondingly substituted piperazines. Reduction of the piperazides IIa - IId and IVa - IVd with diborane in situ in tetrahydrofuran afforded corresponding 1-substituted 4-(3-pyridylmethyl)piperazines IIIa - IIId and Va - Vd. Whereas the alkylation of 1-(2-pyrimidinyl)piperazine with 2-(chloromethyl)pyridine in ethanol in the presence of triethylamine resulted in compounds Ve, compound Vf was obtained by the addition reaction of 1-(3-pyridylmethyl)piperazine to acrylamide. The piperazides VIe and VIf were prepared by reactions of 2-(3-pyridyl)acetic acid with 1-(2-pyrimidinyl)piperazine or 3-(1-piperazinyl)propionamide in N,N-dimethylformamide in the presence 1,1'-carbonyldiimidazole. A similar procedure starting from nicotinic acid afforded the piperazide IVf. Compounds Vc and Vd showed significant affinity for the histamine H1-receptors (inhibition of binding of 2 nmol/l [3H]mepyramine in membranes from the rat brain: Vc, IC50 = 28 nmol/l; Vd, IC50 = 148 nmol/l). They also proved active in test of histamine aerosol in guinea pigs (PD50 = 4.1 mg/kg p.o. for compound Vc and 2.4 for compound Vd). Results of a more detailed pharmacological testing of these compounds will be published elsewhere.
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2

Gettys, Kristen, Zhishi Ye, and Mingji Dai. "Recent Advances in Piperazine Synthesis." Synthesis 49, no. 12 (April 25, 2017): 2589–604. http://dx.doi.org/10.1055/s-0036-1589491.

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Piperazine ranks as the third most common N-heterocycle appearing in small-molecule pharmaceuticals. This review highlights recent advances in methods development for the construction of the piperazine­ ring system with particular emphasis on preparing carbon-substituted piperazines.1 Introduction2 Reduction of (Di)ketopiperazine3 N-Alkylation4 Transition-Metal-Catalyzed/Mediated Piperazine Synthesis4.1 The SnAP and SLAP Methods4.2 Palladium-Catalyzed Cyclization4.3 Gold-Catalyzed Cyclization4.4 Other Metal-Catalyzed/Mediated Cyclization4.5 Borrowing Hydrogen Strategy4.6 Imine Reductive Cyclization5 Reduction of Pyrazines6 Miscellaneous7 Conclusion
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3

Hafeez, Freeha, Ameer Fawad Zahoor, Azhar Rasul, Asim Mansha, Razia Noreen, Zohaib Raza, Kulsoom Ghulam Ali, Ali Irfan, and Gamal A. El-Hiti. "Ultrasound-Assisted Synthesis and In Silico Modeling of Methanesulfonyl-Piperazine-Based Dithiocarbamates as Potential Anticancer, Thrombolytic, and Hemolytic Structural Motifs." Molecules 27, no. 15 (July 26, 2022): 4776. http://dx.doi.org/10.3390/molecules27154776.

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Piperazine-based dithiocarbamates serve as important scaffolds for numerous pharmacologically active drugs. The current study investigates the design and synthesis of a series of dithiocarbamates with a piperazine unit as well as their biological activities. Under ultrasound conditions, the corresponding piperazine-1-carbodithioates 5a–5j were synthesized from monosubstituted piperazine 2 and N-phenylacetamides 4a–4j in the presence of sodium acetate and carbon disulfide in methanol. The structures of the newly synthesized piperazines were confirmed, and their anti-lung carcinoma effects were evaluated. A cytotoxic assay was performed to assess the hemolytic and thrombolytic potential of the synthesized piperazines 5a–5j. The types of substituents on the aryl ring were found to affect the anticancer activity of piperazines 5a–5j. Piperazines containing 2-chlorophenyl (5b; cell viability = 25.11 ± 2.49) and 2,4-dimethylphenyl (5i; cell viability = 25.31 ± 3.62) moieties demonstrated the most potent antiproliferative activity. On the other hand, piperazines containing 3,4-dichlorophenyl (5d; 0.1%) and 3,4-dimethylphenyl (5j; 0.1%) rings demonstrated the least cytotoxicity. The piperazine with the 2,5-dimethoxyphenyl moiety (5h; 60.2%) showed the best thrombolytic effect. To determine the mode of binding, in silico modeling of the most potent piperazine (i.e., 5b) was performed, and the results were in accordance with those of antiproliferation. It exhibits a similar binding affinity to PQ10 and an efficient conformational alignment with the lipophilic site of PDE10A conserved for PQ10A.
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4

Durand, Carolina, and Michal Szostak. "Recent Advances in the Synthesis of Piperazines: Focus on C–H Functionalization." Organics 2, no. 4 (October 8, 2021): 337–47. http://dx.doi.org/10.3390/org2040018.

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Piperazine ranks as the third most common nitrogen heterocycle in drug discovery, and it is the key component of several blockbuster drugs, such as Imatinib (also marketed as Gleevec) or Sildenafil, sold as Viagra. Despite its wide use in medicinal chemistry, the structural diversity of piperazines is limited, with about 80% of piperazine-containing drugs containing substituents only at the nitrogen positions. Recently, major advances have been made in the C–H functionalization of the carbon atoms of the piperazine ring. Herein, we present an overview of the recent synthetic methods to afford functionalized piperazines with a focus on C–H functionalization.
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5

Yadav, Pradeep, and Y. C. Joshi. "Synthesis and Spectral Study of Novel Norfloxacin Derivatives." E-Journal of Chemistry 5, s2 (2008): 1154–58. http://dx.doi.org/10.1155/2008/357073.

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Reaction of [1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-quinolone-3-carboxylic acid (norfloxacin) with thiazole / benzothiazole diazonium chloride to get new piperazine substituted norfloxacin derivative. These norfloxacin derivatives were further condensed with variousβ-diketone to get novel acid derivatives of 1-Ethyl-6-fluoro-4-oxo-7- [4 (thiazol-2-yldiazenyl)-piperzin-1-yl]-1,4-dihydro-quinoline-3-carboxylic acid (6a-e) and 7-(4-(benzo[d]thiazol-2-yldiazenyl)piperazin-1-yl)-1-ethyl-6-fluoro-4-oxo-1, 4-dihydroquinoline-3-carboxylic acid (6 f-j). Structures of these compounds were established on the basis of spectral studies viz. IR,1H NMRetc.
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6

O’Malley, Karen, and Keith Vaughan. "Synthesis and Characterization of a Series of 1-Aryl-4-[Aryldiazenyl]-piperazines. Part II1. 1-Aryl-4-(2-Aryl-1-Diazenyl)-piperazines with Fluoro-, chloro-, Methyl-, Cyano- and Acetyl Substituents in The 1-Aryl Group." Open Chemistry Journal 3, no. 1 (May 31, 2016): 42–55. http://dx.doi.org/10.2174/1874842201603010042.

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This paper reports the synthesis and characterization of eight series of 1-aryl-4-(2-aryl-1-diazenyl)-piperazines (12 to 19). Several series of these triazenes have been synthesized by the diazotization of a primary arylamine followed by diazonium coupling with a secondary arylpiperazine . The arylpiperazines used in this study are: 1-phenylpiperazine, 1-(4-fluorophenyl-)piperazine, 1-(4-chlorophenyl-)piperazine, 1-(3,4-dichlorophenyl-)piperazine, 1-(2-methylphenyl-)-piperazine, 1-(4-acetophenyl-)-piperazine, 1-(2-pyridyl-)piperazine and 2-cyanophenylpiperazine. These new triazenes (series 12-19) have been identified with a cocktail of contemporary spectroscopic techniques, notably infra-red and nuclear magnetic spectroscopy, supported by high resolution electron ionization mass spectrometry.
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7

Little, Vanessa Renee, and Keith Vaughan. "Synthesis and characterization of several series of 4-acyl-1-[2-aryl-1-diazenyl]piperazines." Canadian Journal of Chemistry 92, no. 9 (September 2014): 838–48. http://dx.doi.org/10.1139/cjc-2014-0242.

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Five series of a novel class of 4-acyl-1-[2-aryl-1-diazenyl]piperazines have been synthesized and characterized: the 4-acetyl-1-[2-aryl-1-diazenyl]piperazines [series 1]; the 4-cyclohexylcarbonyl-1-[2-aryl-1-diazenyl]piperazines [series 2]; the 4-benzoyl-1-[2-aryl-1-diazenyl]piperazines [series 3]; the benzyl 4-[2-aryl-1-diazenyl]-1-piperazinecarboxylates [series 4]; and the t-butyl 4-[2-aryl-1-diazenyl]-1-piperazinecarboxylates [series 5]. The compounds were synthesized by diazotization of a primary aromatic amine and subsequent coupling to an appropriate secondary amine: 1-acetylpiperazine [series 1]; 1-(cyclohexylcarbonyl)-piperaizine [series 2]; 1-benzoylpiperazine [series 3]; benzyl 1-piperazinecarboxylate [series 4]; and t-butyl piperazine-1-carboxylate (1-BOC-piperazine) [series 5]. The compounds of series 1–5 were characterized by 1H NMR, 13C NMR, high-resolution MS and IR spectroscopy. The model compounds 1,4-di[2-aryl-1-diazenyl]piperazines, and ethyl 4-[2-aryl-1-diazenyl]-1-piperazinecarboxylates were used to facilitate the assignment of the chemical shifts specific to the piperazine ring carbons. HSQC spectra of select compounds established the correlation between proton and carbon resonance signals.
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8

Penjisevic, Jelena, Vladimir Sukalovic, Deana Andric, Goran Roglic, Irena Novakovic, Vukic Soskic, and Sladjana Kostic-Rajacic. "Synthesis, biological evaluation and docking analysis of substituted piperidines and (2-methoxyphenyl)piperazines." Journal of the Serbian Chemical Society 81, no. 4 (2016): 347–56. http://dx.doi.org/10.2298/jsc151021097p.

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A series of sixteen novel substituted piperidines and (2-methoxyphenyl)piperazines were synthesized, starting from the key intermediates 1-(2-methoxyphenyl)-4-(piperidin-4-yl)piperazine and 1-(2-methoxyphenyl)-4-(piperidin-4-ylmethyl)piperazine. Biological evaluation of the synthesized compounds was pointed out for seven compounds, of which 1-(2-methoxyphenyl)-4-{[1-(2-nitrobenzyl)piperidin-4-yl]methyl}piperazine had the highest affinity for the dopamine D2 receptor. For all seven selected compounds docking analysis was performed in order to establish their structure-to-activity relationship.
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9

Kafka, Stanislav, Jan Čermák, Tomáš Novák, František Pudil, Ivan Víden, and Miloslav Ferles. "Syntheses of piperazines substituted on the nitrogen atoms with allyl, propyl, 2-hydroxypropyl and 3-hydroxypropyl groups." Collection of Czechoslovak Chemical Communications 50, no. 5 (1985): 1201–11. http://dx.doi.org/10.1135/cccc19851201.

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The paper describes synthesis of 1,4-diallylpiperazine (I), 1-allylpiperazine (III), 1-propylpiperazine (IV), 1-(1-piperazinyl)-2-propanol (V), 3-(1-piperazinyl)-1-propanol (VI), 1-allyl-4-propylpiperazine (VII), 1-(4-allyl-1-piperazinyl)-2-propanol (VIII), 3-(4-allyl-1-piperazinyl)-1-propanol (IX), 1,4-dipropylpiperazine (X), 1-(4-propyl-1-piperazinyl)-2-propanol (XI), 3-(4-propyl-1-piperazinyl)-1-propanol (XII), 1,4-bis(2-hydroxypropyl)piperazine (XIII), 3-[4-(2-hydroxypropyl)-1-piperazinyl]-1-propanol (XIV) and 1,4-bis(3-hydroxypropyl)piperazine (XV). Retention indices of I-XV reported and mass spectra of the compounds are discussed.
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10

Magriotis, Plato A. "Recent progress toward the asymmetric synthesis of carbon-substituted piperazine pharmacophores and oxidative related heterocycles." RSC Medicinal Chemistry 11, no. 7 (2020): 745–59. http://dx.doi.org/10.1039/d0md00053a.

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The piperazine drugs are mostly N-substituted compared to only a few C-substituted drugs. To explore this unknown chemical space, asymmetric syntheses of C-substituted piperazines is the subject of this review.
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11

Periasamy, Mariappan, Boda Venkanna, Miriyala Nagaraju, and Lakavathu Mohan. "Methods for the Synthesis of Piperazine Derivatives Containing a Chiral Bi-2-naphthyl Moiety." Synthesis 52, no. 01 (October 1, 2019): 127–34. http://dx.doi.org/10.1055/s-0037-1610731.

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Piperazine derivatives containing 1,1′-bi-2-naphthyl moiety were synthesized starting from 2,2′-dimethoxy-1,1′-bi-naphthalene via acylation using ethyl chlorooxoacetate and subsequent condensation with 1,2-diamines followed by reduction of the corresponding dihydro-2-piperazinone intermediate using the NaBH4/I2 reagent system. The corresponding chiral piperazine derivatives containing bi-2-napthyl moiety was synthesized by asymmetric reduction of ethyl dimethoxy-bi-2-naphthyloxoacetate by chiral oxazoborolidine catalyst prepared in situ using S-diphenylprolinol (S-DPP), B(OCH3)3 and H3B·THF. The resulting diols were mesylated and cyclized using 1,2-diamines to obtain the corresponding chiral piperazine derivatives.
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12

Chamakuri, Srinivas, Sunny Ann Tang, Kevin A. Tran, Shiva Krishna Reddy Guduru, Peter K. Bolin, Kevin R. MacKenzie, and Damian W. Young. "A Concise Synthetic Method for Constructing 3-Substituted Piperazine-2-Acetic Acid Esters from 1,2-Diamines." Molecules 27, no. 11 (May 25, 2022): 3419. http://dx.doi.org/10.3390/molecules27113419.

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We report a short synthetic route for synthesizing 2,3-substituted piperazine acetic acid esters. Optically pure amino acids were efficiently converted into 1,2-diamines that could be utilized to deliver the title 2,3-substituted piperazines in five steps with a high enantiomeric purity. The novel route facilitated, for the first time, the synthesis of 3-phenyl substituted-2-piperazine acetic acid esters that were difficult to achieve using other methods; however, in this case, the products underwent racemization.
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13

Little, Vanessa Renée, Reid Tingley, and Keith Vaughan. "Triazene derivatives of (1,x)-diazacycloalkanes. Part III. Synthesis and characterization of a series of 1,4-di[2-aryl-1-diazenyl]piperazines." Canadian Journal of Chemistry 83, no. 5 (May 1, 2005): 471–76. http://dx.doi.org/10.1139/v05-064.

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Reaction of a series of diazonium salts with piperazine in a 2:1 molar ratio affords excellent yields of the 1,4-di-[2-aryl-1-diazenyl]piperazines (3), which have been characterized by IR and NMR spectroscopy. Structural characterization is supported by elemental analysis or by mass spectrometry with accurate mass measurement of the molecular ion. The protons of the piperazine ring hydrogens give rise to a sharp singlet at ca. 4 ppm in the NMR spectra, indicating that the conformational equilibrium in the piperazine ring is rapid on the NMR timescale. The four equivalent carbon atoms of the piperazine ring resonate in the range 46–48 ppm. A variable temperature NMR experiment suggests that there is restricted rotation around the N2—N3 bond of the triazene moiety in 3. The NMR data compares favorably with previous reported data for 1-aryldiazenyl-4-methylpiperazines (1) and 1,4-di-(2-aryldiazen-1-yl)homopiperazines (2b).Key words: triazene, piperazine, diazonium coupling, NMR.
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14

Prabawati, Susy Yunita. "SYNTHESIS OF 1,4-BIS [(1-HYDROXY-4-T-BUTYL-PHENYL) METHYL]PIPERAZINE AS ANTIOXIDANTS." Molekul 11, no. 2 (November 28, 2016): 220. http://dx.doi.org/10.20884/1.jm.2016.11.2.244.

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A study has been conducted to synthesize 1,4-bis [(1-hydroxy-4-t-butyl-phenyl)-methyl]piperazin using phenol derivate and investigate the capability of that compound, as an antioxidant. The synthesis was carried out through Mannich reaction using p-t-butylphenol, paraformaldehyde, and piperazine. The product was characterized by IR and 1H NMR spectroscopic. Testing of antioxidant activity was done with the immersion of DPPH (1,1-diphenyl-2 picrylhydrazyl) free radical method. The product was obtained as a white solid, with a point of 252,7-254,7 ºC and a yield of 65.76%. The test of antioxidant activity with DPPH method showed that 1,4-bis [(1-hydroxy-4-t-butyl-phenyl)-methyl]piperazin had the IC50 values was 0.84 nM. It means that the 1,4- bis[(1-hydroxy-4-t-butyl-phenyl )methyl]piperazine has potential as antioxidants.
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15

Němečková, Dana, Eva Havránková, Jan Šimbera, Richard Ševčík, and Pavel Pazdera. "Simplified Procedure for General Synthesis of Monosubstituted Piperazines—From a Batch Reaction Vessel to a Flow (Microwave) Reactor." Molecules 25, no. 9 (May 6, 2020): 2168. http://dx.doi.org/10.3390/molecules25092168.

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We reported a novel simplified synthetic procedure for the preparation of monosubstituted piperazine derivatives which can now be easily prepared in a one-pot-one-step way from a protonated piperazine with no need of introduction of a protecting group. Reactions, proceeding either at room or higher temperatures in common solvents, involve heterogeneous catalysis by metal ions supported on commercial polymeric resins. A general synthetic scheme was successfully applied to afford a wide range of monosubstituted piperazines. Furthermore, we picked up a set of piperazine derivatives and studied the possibilities of microwave acceleration of given synthetic reactions to make them even more efficient. Our research proceeded from a simple batch technique to the construction of a flow microwave reactor prototype and resulted in promising findings which are summarized and discussed in the article.
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16

Ullah, Nisar. "Synthesis of New 1-Aryl-4-(biarylmethylene)piperazine Ligands, Structurally Related to Adoprazine (SLV313)." Zeitschrift für Naturforschung B 67, no. 1 (January 1, 2012): 75–84. http://dx.doi.org/10.1515/znb-2012-0113.

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A series of new 1-aryl-4-(biarylmethylene)piperazines has been synthesized. These ligands are structurally related to SLV-313, a potential atypical antipsychotic having potent D2 receptor antagonist and 5-HT1A receptor agonist properties. Buchwald-Hartwig coupling reactions of 1-boc-piperazine with appropriate aryl halides and subsequent removal of the boc group rendered arylpiperazines. The reductive amination of the latter with suitable biarylaldehydes accomplished the synthesis of these ligands.
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17

Clifford, Sarah E., Vanny Tiwow, Aleasia Gendron, Marcel Maeder, Monica Rossignoli, Geoffrey A. Lawrance, Peter Turner, Alexander J. Blake, and Martin Schröder. "Complexation of Constrained Ligands Piperazine, N-substituted Piperazines, and Thiomorpholine." Australian Journal of Chemistry 62, no. 10 (2009): 1196. http://dx.doi.org/10.1071/ch09313.

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Complexation of the symmetric cyclic diamine piperazine (1,4-diazacyclohexane) has been examined in dry dimethyl formamide by spectrophotometric titrations (with Cu2+, Ni2+) to define formation constants, and by stopped-flow kinetics to define the complexation rates and reaction pathway. Initial formation of a rarely observed η1-piperazine intermediate occurs in a rapid second-order reactions. This intermediate then undergoes two competing reactions: formation of (chelated) η2-piperazine (ML) or the formation of (bridging) μ-piperazine (in M2L and M2L3, speciation depending on relative concentrations). Protonation constants and formation constants for complexation in water of N-ethylpiperazine and thiomorpholine (1-aza-4-thiocyclohexane, tm) have been determined by potentiometric titration; 1:1 complexes with first-row M2+ display a log K from ~4 to 6, with speciation that suggests chelation of the heterocycles may be involved. Complexation of thiomorpholine has been further probed by the synthesis of PdII complexes. The N-monodentate coordination mode has been confirmed in trans-[Pd(tm)2Br2] by an X-ray crystal structure. Complexation of N-(2-aminoethyl)piperazine to CuII as a bidentate ligand involving the primary and tertiary amines is also defined by an X-ray crystal structure.
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18

Mishra, Vaibhav, and Tejpal Singh Chundawat. "Pd Catalyzed N1/N4 Arylation of Piperazine for Synthesis of Drugs, Biological and Pharmaceutical Targets: An Overview of Buchwald Hartwig Amination Reaction of Piperazine in Drug Synthesis." Current Organic Synthesis 15, no. 2 (April 24, 2018): 208–20. http://dx.doi.org/10.2174/1570179415666171206151603.

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Background: Substituted piperazine heterocycles are among the most significant structural components of pharmaceuticals. N1/N4 substituted piperazine containing drugs and biological targets are ranked 3rd in the top most frequent nitrogen heterocycles in U.S. FDA approved drugs. The high demand of N1/N4 substituted piperazine containing biologically active compounds and U.S. FDA approved drugs, has prompted the development of Pd catalyzed C-N bond formation reactions for their synthesis. Buchwald-Hartwig reaction is the key tool for the synthesis of these compounds. Objective: This review provides strategies for Pd catalyzed C-N bond formation at N1/N4 of piperazine in the synthesis of drugs and biological targets with diverse use of catalyst-ligand system and reaction parameters. Conclusion: It is clear from the review that a vast amount of work has been done in the synthesis of N1/N4 substituted piperazine containing targets under the Pd catalyzed Buchwald-Hartwig amination of aryl halides by using different catalyst-ligand systems. These methods have become increasingly versatile as a result of innovation in catalyst design and improvements in reaction conditions. This review gives an overview of recent utilization of Buchwald-Hartwig amination reaction in drug/target synthesis.
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19

Zhang, Gang, and Courtney C. Aldrich. "Macozinone: revised synthesis and crystal structure of a promising new drug for treating drug-sensitive and drug-resistant tuberculosis." Acta Crystallographica Section C Structural Chemistry 75, no. 8 (July 5, 2019): 1031–35. http://dx.doi.org/10.1107/s2053229619009185.

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Mycobacterium tuberculosis (Mtb), the principal etiological agent of tuberculosis (TB), infects over one-quarter of humanity and is now the leading cause of infectious disease mortality by a single pathogen. Macozinone {2-[4-(cyclohexylmethyl)piperazin-1-yl]-8-nitro-6-(trifluoromethyl)-4H-1,3-benzothiazin-4-one, C20H23F3N4O3S} is a promising new drug for treating drug-sensitive and drug-resistant TB that has successfully completed phase I clinical trials. We report the complete spectroscopic and structural characterization by 1H NMR, 13C NMR, HRMS, IR, and X-ray crystallography. The cyclohexyl moiety is observed to be nearly perpendicular to the core formed by the 1,3-benzothiazin-4-one and piperazine groups. The central piperazine ring adopts a slightly distorted chair conformation caused by sp 2-hybridization of the nitro N atom, which donates into the electron-deficient 1,3-benzothiazin-4-one group.
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20

Abadleh, Mohammed M., Mustafa M. El-Abadelah, Salim S. Sabri, Hanan H. Mohammed, Malek A. Zihlif, and Wolfgang Voelter. "Synthesis and Antitumor Activity of Some N2-(Thien-3-yl)amidrazones." Zeitschrift für Naturforschung B 69, no. 7 (July 1, 2014): 811–16. http://dx.doi.org/10.5560/znb.2014-4062.

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6aA set of new N2-(thien-3-yl)amidrazones (-h) incorporating N-piperazines and related congeners has been synthesized by reacting the hydrazonoyl chloride 4(derived from 3-aminothiophene- 2-carboxylate) with the appropriate sec-cyclic amine. The antitumor activity of these compounds was evaluated on breast cancer (MCF-7) and leukemic (K562) cell lines by a cell viability assay utilizing the tetrazolium dye (MTT). The amidrazone 6d encompassing the N-piperazine moiety, was the most active against MCF-7 and K562 with IC50 of 7.28 and 9:91 μM, respectively.
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21

Sergeev, E. E., L. L. Gogin, T. B. Khlebnikova, E. G. Zhizhina, and Z. P. Pai. "Methods for the catalytic synthesis of piperazine." Kataliz v promyshlennosti 22, no. 1 (January 28, 2022): 67–79. http://dx.doi.org/10.18412/1816-0387-2022-1-67-79.

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An analytical review of the methods used for piperazine synthesis compares two groups of catalytic processes: intermolecular and intramolecular cyclization. Advantages and drawbacks of the existing piperazine synthesis methods are noted; the preferable highly selective processes of intramolecular cyclization using aminoethylethanolamine and diethylenetriamine as well as the single-step processes of intermolecular cyclization using ethylenediamine, mono- and diethanolamine are indicated.
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22

Prasad, H. S. Nagendra, A. P. Ananda, Amogh Mukarambi, Navyatha Prashanth Gaonkar, S. Sumathi, H. P. Spoorthy, and P. Mallu. "Design, synthesis, and anti-bacterial activities of piperazine based phthalimide derivatives against superbug-Methicillin-Resistant Staphylococcus aureus." Current Chemistry Letters 12, no. 1 (2023): 65–78. http://dx.doi.org/10.5267/j.ccl.2022.9.005.

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A series of piperazine-based phthalimide derivatives 5 (a-l) were synthesized and extensively characterized using a variety of spectrum methods, including LC-MS, 1H-NMR, 13C-NMR, and FT-IR. All the derivatives were examined for their physicochemical, pharmacokinetic, bio-activity score, and PASS analysis. The 5e piperazine-based phthalimide derivative demonstrated promising antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA) in the in vitro antibacterial studies. In comparison to streptomycin and bacitracin (10 µg/mL), the minimum inhibitory concentration of 5e against MRSA was discovered to be 45±0.15 micro g/ml. The anti-MRSA activity was validated with membrane damage studies by using SEM, and in silico docking studies were against 3VMT and 6FTB proteins of MRSA. In the toxicity study, 5e derivatives were evaluated against L6 cell lines. The results of the studies show the synthesized 2-(2-(4-((4-chlorophenyl) sulfonyl) piperazin-1-yl) ethyl) isoindoline-1,3-dione (5e) can be used for the development of anti-MRSA drugs.
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23

Patel, Nalini, Vaishali Karkhanis, and Pinkal Patel. "Synthesis and Biological Evaluation of Some Piperazine Derivatives as Anti-Inflammatory Agents." Journal of Drug Delivery and Therapeutics 9, no. 4-s (August 15, 2019): 353–58. http://dx.doi.org/10.22270/jddt.v9i4-s.3327.

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Some 1-((4-methylpiperazin-1yl)methyl)-1H-benzo[d]imidazole & 1-((4-phenylpiperazin-1yl)methyl)-1H-benzo[d]imidazole derivatives were synthesized through reaction of 1-substituted piperazines with different benzimidazole derivatives in methanol yielded the corresponding mannich bases (42-a to 42-i). All the synthesized compounds were elucidated by IR, 1H NMR and MASS spectroscopy. They were tested for anti-inflammatory activity using in-vivo (Carrageenan- induced rat paw edema model) method at a dose of 50mg/kg. result showed that compounds 42-c, 42-d and 42-h were found to be most potent in series. Keywords: 1,4-disubstituted Piperazine, Anti-inflammatory, Mannich Base.
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24

Little, Vanessa Renée, and Keith Vaughan. "Synthesis and characterization of a series of 1-methyl-4-[2-aryl-1-diazenyl]piperazines and a series of ethyl 4-[2-aryl-1-diazenyl]-1-piperazinecarboxylates." Canadian Journal of Chemistry 82, no. 8 (August 1, 2004): 1294–303. http://dx.doi.org/10.1139/v04-081.

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1-Methylpiperazine was coupled with a series of diazonium salts to afford the 1-methyl-4-[2-aryl-1-diazenyl]piperazines (2), a new series of triazenes, which have been characterized by 1H and 13C NMR spectroscopy, IR spectroscopy, and elemental analysis. Assignment of the chemical shifts to specific protons and carbons in the piperazine ring was facilitated by comparison with the chemical shifts in the model compounds piperazine and 1-methylpiperazine and by a HETCOR experiment with the p-tolyl derivative (2i). A DEPT experiment with 1-methylpiperazine (6) was necessary to distinguish the methyl and methylene groups in 6, and a HETCOR spectrum of 6 enabled the correlation of proton and carbon chemical shifts. Line broadening of the signals from the ring methylene protons is attributed to restricted rotation around the N2-N3 bond of the triazene moiety in 2. The second series of triazenes, the ethyl 4-[2-phenyl-1-diazenyl]-1-piperazinecarboxylates (3), have been prepared by similar diazonium coupling to ethyl 1-piperazinecarboxylate and were similarly characterized. The chemical shifts of the piperazine ring protons are much closer together in series 3 than in series 2, resulting in distortion of the multiplets for these methylenes. It was noticed that the difference between these chemical shifts in 3 exhibited a linear free energy relationship with the Hammett substituent constants for the substituents in the aryl ring. Key words: triazene, piperazine, diazonium coupling, NMR, HETCOR, linear free energy relationship.
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25

Dileep, Kommula, and M. Murty. "Aqueous, One-Pot, Three-Component Reaction for Efficient Synthesis of 2-[4-(Arylsulfonyl)piperazin-1-yl]-1,3-benzothiazole, ‑1H-benzimidazole, or -1,3-benzoxazole Derivatives." Synlett 28, no. 17 (August 3, 2017): 2295–98. http://dx.doi.org/10.1055/s-0036-1590972.

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A simple and efficient synthetic protocol has been developed involving a one-pot three-component reaction of a 2-chlorobenzazole, piperazine, and an arenesulfonyl chloride under aqueous conditions at room temperature in the absence of a catalyst, ligand, or base. By using this protocol, a variety of 2-[4-(arylsulfonyl)piperazin-1-yl]-1,3-benzothiazole, -1H-benzimidazole, and -1,3-benzoxazole derivatives were synthesized in excellent yields.
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26

Cai, Dong, ZhiHua Zhang, Yufan Meng, KaiLi Zhu, LiYi Chen, ChangXiang Yu, ChangWei Yu, ZiYi Fu, DianShen Yang, and YiXia Gong. "Efficient synthesis of piperazinyl amides of 18β-glycyrrhetinic acid." Beilstein Journal of Organic Chemistry 16 (April 21, 2020): 798–808. http://dx.doi.org/10.3762/bjoc.16.73.

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In the present study, a practical method to prepare piperazinyl amides of 18β-glycyrrhetinic acid was developed. Two main procedures for the construction of important intermediate 8 are discussed. One procedure involves the amidation of 1-Boc-piperazine with 3-acetyl-18β-glycyrrhetinic acid, prepared by the reaction of 18β-glycyrrhetinic acid with acetic anhydride without any solvent at 130 °C. The other procedure to prepare compound 8 involves the amidation of 18β-glycyrrhetinic acid followed by the esterification with acetic anhydride. Finally, compound 8 underwent N-Boc deprotection to prepare product 4. To ascertain the scope of the reaction, another C-3 ester derivative 17 was tested under the optimized reaction conditions. Furthermore, the reasons for the appearance of byproducts were elucidated. Crystallographic data of a selected piperazinyl amide is reported.
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27

Andric, Deana, Gordana Tovilovic, Goran Roglic, Djurdjica Vaskovic, Vukic Soskic, Mirko Tomic, and Sladjana Kostic-Rajacic. "Synthesis and pharmacological evaluation of several N-(2-nitrophenyl) piperazine derivatives." Journal of the Serbian Chemical Society 72, no. 5 (2007): 429–35. http://dx.doi.org/10.2298/jsc0705429a.

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Six newly synthesized heterocyclic (2-nitrophenyl)piperazines, with a specific structure of the heteroaryl group, whichmimics the catechol moiety of dopamine (benzimidazoles and substituted benzimidazoles), were evaluated for their binding affinity to rat dopamine (DA), serotonin (5-HT) and _1 receptors. All compounds with a benzimidazole group had a 5-HT2A/D2 receptors binding ratio characteristic for atypical neuroleptics (>1, pK i values). Compound 7c, 4-bromo-6-{2-_4-(2-nitrophenyl)piperazin- 1-yl_ethyl}-1H-benzimidazole, expressed higher affinities for all receptor classes than clozapine. Also, it exhibited the best characteristic for atypical neuroleptics and presents a compound with the best profile for further in vivo investigations.
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28

Hu, Fan, and Weike Su. "An investigation of the synthesis of vilazodone." Journal of Chemical Research 44, no. 3-4 (December 17, 2019): 243–47. http://dx.doi.org/10.1177/1747519819893293.

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A novel synthetic route toward vilazodone is described by using 4-cyanoaniline and 5-bromo-2-hydroxybenzaldehyde as starting materials, with an overall yield of 24% and 99% purity. First, the intermediate (3-(4-chlorobutyl)-1 H-indole-5-carbonitrile) is synthesized via diazotization of 4-cyanoaniline, followed by Fischer indole cyclization with 6-chlorohexanal. Subsequently, another intermediate, 5-(piperazin-1-yl)benzofuran-2-carboxamide, is generated via aromatic nucleophilic substitution of 5-bromobenzofuran-2-carboxamide with piperazine. Finally, vilazodone is obtained via nucleophilic substitution of the above two key intermediates by treatment with Et3N/K2CO3. In comparison to the original process, this route avoids the use of expensive and toxic reagents and resolves issues such as safety, environmental concerns, and high costs.
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29

Vejdělek, Zdeněk, and Miroslav Protiva. "1-(4-Cyclopentylphenyl)piperazine and its 4-substituted derivatives; Synthesis and biological screening." Collection of Czechoslovak Chemical Communications 52, no. 7 (1987): 1834–40. http://dx.doi.org/10.1135/cccc19871834.

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Heating the hydrochlorides of 4-cyclopentylaniline and diethanolamine to 250 °C gave 1-(4-cyclopentylphenyl)piperazine (I). Acylation of I with ethyl formate and the corresponding acyl chlorides gave the amides II, VI, and VII which were reduced with lithium aluminium hydride to the piperazines III, VIII, and IX. Treatment of I with benzyl chloride and with 4-chloro-1-(4-fluorophenyl)butan-1-one under different conditions led to compounds IX and XI. Addition reaction of I to 1,2-epoxybutane resulted in the amino alcohol V. The products showed marginal tranquillizing activity (especially compound VIII), some antimicrobial activity in vitro and some anthelmintic activity.
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30

Li, Wen, Shu-Yi Chen, Wei-Nan Hu, Mei Zhu, Jia-Min Liu, Yi-Hong Fu, Zhen-Chao Wang, and Gui-Ping OuYang. "Design, synthesis, and biological evaluation of quinazoline derivatives containing piperazine moieties as antitumor agents." Journal of Chemical Research 44, no. 9-10 (March 17, 2020): 536–42. http://dx.doi.org/10.1177/1747519820910384.

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A series of novel quinazoline derivatives containing piperazine analogs are synthesized via substitution reactions with 6,7-disubstituted 4-chloroquinazoline and benzyl piperazine (amido piperazine). Potent antiproliferative activities are observed against A549, HepG2, K562, and PC-3 with N-(3-chlorophenyl)-2-(4-(7-methoxy-6-(3-morpholino-propoxy)quinazoline-4-yl)piperazine-1-yl)acetamidename C9 showing excellent activity. This active derivative was screened for cell migration ability, proliferation effects, and apoptosis against A549 and PC-3 cells, with the result showing biological activity almost equal to that of the control gefitinib.
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31

Tang, Yan-Ling, Yong-Kun Li, Min-Xin Li, Hui Gao, Xiao-Bi Yang, and Ze-Wei Mao. "Synthesis of New Piperazine Substituted Chalcone Sulphonamides as Antibacterial Agents." Current Organic Synthesis 17, no. 2 (May 8, 2020): 136–43. http://dx.doi.org/10.2174/1570179417666191227115207.

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Background: Infection is a global threat to human health, and there is an urgent need to develop new effective antibacterial drugs to treat bacterial infections. Objective: To study the antibacterial activity of piperazine substituted chalcone sulphonamides. Materials and Methods: A series of novel piperazine substituted chalcone sulphonamides have been prepared, and in vitro antibacterial activity against Staphylococcus aureus, Bacillus subtilis and Escherichia coli strains were evaluated. Results: The results showed that derivatives 6a, 6c and 6h displayed good antibacterial activity against Bacillus subtilis with MIC values of 4.0-8.0 mg/mL. Conclusion: Piperazine substituted chalcone sulphonamides may be used as potential antibacterial agents.
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32

Khazaee, Asma, Roya Jahanshahi, Sara Sobhani, Jørgen Skibsted, and José Miguel Sansano. "Immobilized piperazine on the surface of graphene oxide as a heterogeneous bifunctional acid–base catalyst for the multicomponent synthesis of 2-amino-3-cyano-4H-chromenes." Green Chemistry 22, no. 14 (2020): 4604–16. http://dx.doi.org/10.1039/d0gc01274b.

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A green method for the efficient synthesis of 2-amino-3-cyano-4H-chromenes using immobilized piperazine on the surface of graphene oxide (piperazine-GO) as a new heterogeneous bifunctional acid–base catalyst is developed.
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33

Patel, H. S., H. D. Desai, and H. J. Mistry. "Synthesis and Antimicrobial Activity of Some New Piperazine Derivaties Containing Aryl Sulfonyloxy Group." E-Journal of Chemistry 1, no. 2 (2004): 93–98. http://dx.doi.org/10.1155/2004/732420.

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NovelN-substituted piperazine derivatives containing sulfonyloxy aniline moiety have been prepared. The various 4-sulfonyloxy aniline (SA) derivatives (2a-h) have been prepared by the condensation reaction ofN-Acetyl Sulfanilyl chloride (ASC) and sodium phenates followed by hydrolysis. The SA derivatives are then reacted with chloro acetyl chloride to give corresponding (N-Chloroacetyl) derivatives (3a-h). These derivatives are then reacted withN-phenyl piperazine to yield the corresponding piperazine derivatives (4a-h).
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34

SARI, Sait, and Mehmet YILMAZ. "Synthesis and characterization of piperazine-substituted dihydrofuran derivatives viaMn(OAc)3 mediated radical cyclizations." TURKISH JOURNAL OF CHEMISTRY 44, no. 5 (October 26, 2020): 1303–13. http://dx.doi.org/10.3906/kim-2003-23.

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The aim of this study is to synthesize novel piperazine-containing dihydrofuran compounds (3a-n)from radical additions and cyclizations of diacyl and alkyl-acyl piperazine derivatives (1a-h) with 1,3-dicarbonyl compounds (2a-c) mediated by Mn(OAc)3 for the first time. From the reactions of 1a-c with dimedone (2a);1a, 1c, and 1d with acetylacetone (2b); and 1a with ethylacetoacetate(2c) ,the dihydrofuran-piperazine compounds 3a-c, 3d-f, and 3g were obtained in medium to high yields (31%–81%), respectively. In addition, dihydrofuran-piperazine compounds 3h-j and 3k-n were prepared at low to medium yields (20%–40%) from the reactions of 1e-g with 2a and 1e-h with 2c, respectively.
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35

Derkaoui, Samira, Djamal Eddine Kherroub, and Mohammed Belbachir. "Green synthesis, anionic polymerization of 1,4-bis(methacryloyl)piperazine using Algerian clay as catalyst." Green Processing and Synthesis 8, no. 1 (January 28, 2019): 611–21. http://dx.doi.org/10.1515/gps-2019-0031.

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Abstract In this work, a chain of reactions has been proposed as a new heterogeneous technique, based on the use of natural treated clays as an environmentally friendly catalysts for the synthesis of poly(1,4-bis(methacryloyl)piperazine). We first synthesized the monomer; 1,4-bis(methacryloyl)piperazine (NBMP) in bulk (without solvent) by the condensation of heterocyclic secondary amines piperazine with methacrylic anhydride catalyzed by maghnite-H+ at room temperature during 2 h. After that, we have polymerized anionically the obtained NBMP in an ice bath using anionic catalyst maghnite-Na+ at 0°C, the reaction took place in 24 h. The poly(1,4-bis(methacryloyl)piperazine) and NBMP structure was characterized and confirmed by infrared spectroscopy, 1H and 13C nuclear magnetic resonance spectroscopies. Thermal properties of the polymer were determined using thermogravimetric analysis. The yield of the reaction was 72% and 59% for the monomer and polymer synthesis respectively. The effect of the weight content of the catalyst on the reaction yield was studied. A polymerization mechanism has been suggested showing the role of maghnite as a catalyst during the reaction courses.
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36

Bobtaina, Eman, Enise Ece Gurdal, Irem Durmaz, Rengul Cetin Atalay, and Mine Yarim. "Synthesis and Cytotoxicity Studies on Novel Piperazinylacetamides." Letters in Drug Design & Discovery 16, no. 1 (November 1, 2018): 45–51. http://dx.doi.org/10.2174/1570180815666180501124009.

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Background: In this study, nine novel compounds, bearing N-[2-(4-substituted piperazine-1-yl)acetyl]-N’-[bis-(4-fluorophenyl)methyl]piperazine structures were synthesized. Methods: Their cytotoxic properties were evaluated in vitro by NCI-60 Sulforhodamine B (SRB) assay against human cancer cell lines: Huh7 (hepatocellular), MCF7 (breast) and HCT116 (colorectal). Results and Conclusion: According to the activity data, most of the compounds are more cytotoxic than 5-fluorouracil against Huh7 and HCT116 cancer cell lines.
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37

Podturkina, Alexandra V., Nikolai S. Li-Zhulanov, Konstantin P. Volcho, and Nariman F. Salakhutdinov. "(1R,2R,6S)-2(4-(4-Isopropylbenzyl)piperazin-1-yl)-3-methyl-6-(prop-1-en-2-yl)cyclohex-3-enol." Molbank 2023, no. 1 (January 12, 2023): M1546. http://dx.doi.org/10.3390/m1546.

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Parkinson’s disease (PD) is a progressive neurodegenerative disorder mainly characterized by movement dysfunction. Earlier, it was found that (1R,2R,6S)-3-methyl-6-(prop-1-en-2-yl)cyclohex-3-ene-1,2-diol (Prottremin) demonstrated antiparkinsonian activity in vivo on different animal models of PD. The paper presents synthesis of new Prottremin derivative, (1R,2R,6S)-2(4-(4-isopropylbenzyl)piperazin-1-yl)-3-methyl-6-(prop-1-en-2-yl)cyclohex-3-enol. The derivative was obtained by epoxide ring opening reaction with 1-(4-isopropylbenzyl)piperazine. The product yield was 48% after purification.
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38

Patel, Divyesh, Rahul Patel, Premlata Kumari, and Navin B. Patel. "Synthesis of s-Triazine-Based Thiazolidinones as Antimicrobial Agents." Zeitschrift für Naturforschung C 67, no. 3-4 (April 1, 2012): 108–22. http://dx.doi.org/10.1515/znc-2012-3-402.

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5A novel series of thiazolidinone derivatives, namely 4-{4-dimethylamino-6-[4-oxo- 2-phenyl-5-(4-pyridin-2-yl-piperazin-1-ylmethyl)-thiazolidin-3-yl]-[1,3,5]-triazin-2-yloxy}- 1-methyl-1H-quinolin-2-ones, have been synthesized from the key intermediate 4-(4-amino- 6-dimethylamino-[1,3,5]-triazin-2-yloxy)-1-methyl-1H-quinolin-2-one (). Compound 5 was condensed with various aldehydes to give Schiff base derivatives, which after cyclization gave thiazolidinones that were linked with 1-pyridin-2-yl-piperazine to obtain the target compounds. The newly synthesized compounds were evaluated for their antimicrobial activity against eight bacteria (Staphylococcus aureus, Bacillus cereus, Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Salmonella typhi, Proteus vulgaris, Shigella flexneri) and four fungi (Aspergillus niger, Candida albicans, Aspergillus fumigatus, Aspergillus clavatus)
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39

Takeuchi, Seiji, Yoshiaki Ohgo, Norikazu Miyoshi, Chung-gi Shin, and Yasuchika Yonezawa. "Asymmetric Synthesis of a Piperazine Alkaloid." HETEROCYCLES 31, no. 11 (1990): 2073. http://dx.doi.org/10.3987/com-90-5573.

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40

Fathalla, Walid, and Pavel Pazdera. "Convenient Synthesis of Piperazine Substituted Quinolones." Journal of Heterocyclic Chemistry 54, no. 6 (September 8, 2017): 3481–89. http://dx.doi.org/10.1002/jhet.2971.

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41

Sharma, Anjali, Sharad Wakode, Faizana Fayaz, Shaik Khasimbi, Faheem H. Pottoo, and Avneet Kaur. "An Overview of Piperazine Scaffold as Promising Nucleus for Different Therapeutic Targets." Current Pharmaceutical Design 26, no. 35 (October 16, 2020): 4373–85. http://dx.doi.org/10.2174/1381612826666200417154810.

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Piperazine scaffolds are a group of heterocyclic atoms having pharmacological values and showing significant results in pharmaceutical chemistry. Piperazine has a flexible core structure for the design and synthesis of new bioactive compounds. These flexible heterogenous compounds exhibit various biological roles, primarily anticancer, antioxidant, cognition enhancers, antimicrobial, antibacterial, antiviral, antifungal, antiinflammatory, anti-HIV-1 inhibitors, antidiabetic, antimalarial, antidepressant, antianxiety and anticonvulsant activities, etc. In the past few years, researchers focused on the therapeutic profile of piperazine synthons for different biological targets. The present review highlights the development in designing pharmacological activities of nitrogen-containing piperazine moiety as a therapeutic agent. The extensive popularity of piperazine as a drug of abuse and their vast heterogeneity research efforts over the last years motivated the new investigators to further explore this area.
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42

Borys, Krzysztof M., Dorota Wieczorek, Magdalena Tarkowska, Agnieszka Jankowska, Jacek Lipok, and Agnieszka Adamczyk-Woźniak. "Mechanochemical synthesis of antifungal bis(benzoxaboroles)." RSC Advances 10, no. 61 (2020): 37187–93. http://dx.doi.org/10.1039/d0ra07767d.

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43

Vejdělek, Zdeněk, and Miroslav Protiva. "N-(piperazinoacyl) and N-(piperazinoalkyl) derivatives of 4-cyclopentylaniline and related compounds: Synthesis and pharmacological screening." Collection of Czechoslovak Chemical Communications 51, no. 7 (1986): 1494–502. http://dx.doi.org/10.1135/cccc19861494.

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Five N-(4-cyclopentylphenyl)haloalkanecarboxamides were reacted with 1-methylpiperazine and 1-(2-hydroxyethyl)piperazine to give the corresponding N-(4-cyclopentylphenyl)piperazinoalkanecarboxamides Iab -Vab. Their reduction with lithium aluminium hydride afforded the triamines VIIab - XIab. Acylation of the N-(4-methylpiperazino)alkyl-4-cyclopentylanilines Xa and XIa with propionyl chloride resulted in the propionanilides XIVa and XVa, whereas a similar reaction of the N-(4-(2-hydroxyethyl)piperazino)alkyl-4-cyclopentylanilines VIIb and IXb - XIb produced the propionoxypropionanilides XIIc - XVc. Ethanolysis of these compounds afforded corresponding hydroxypropionanilides XIIb - XVb. Many of the basic amides showed local anaesthetic and papaverine-like antispasmodic activity. The propionanilides XIIb, XIVc, and XVa proved interesting analgesic effects in the peritoneal test in mice.
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44

Kracht, Daniel, Susumu Saito, and Bernhard Wünsch. "Synthesis of 1,4-Diazabicyclo[3.3.1]nonan-6-ones." Australian Journal of Chemistry 62, no. 12 (2009): 1684. http://dx.doi.org/10.1071/ch09206.

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1,4-Diazabicyclo[3.3.1]nonanes (aza-morphans) represent conformationally constrained piperazine derivatives. Herein, we report a six-step synthesis of the benzyl and allyl substituted bicyclic ketones 3a and 3b, which represent interesting building blocks for the synthesis of conformationally restricted receptor ligands. The key steps of the synthesis are the regioselective addition of ethyl acrylate to the piperazine 8, the sodium hexamethyldisilazide-induced Dieckmann cyclization of the diesters 10, and the decarboxylation of the enol esters 11 with dilute HCl. The complete sequence is only successful when a benzyl (10a) or allyl moiety (10b) is attached to N-1, since the tosyl derivative 10f failed to give a Dieckmann cyclization product, and the decarboxylation failed with the acyl derivatives 11c and 11d.
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45

Costișor, Otilia, Ramona Tudose, Ingo Pantenburg, and Gerd Meyer. "A New Copper (II) Complex with the N,N'-Bis(antipyryl-4-methyl)-piperazine (BAMP) Ligand: [Cu(BAMP)](ClO4)2." Zeitschrift für Naturforschung B 57, no. 12 (December 1, 2002): 1454–60. http://dx.doi.org/10.1515/znb-2002-1218.

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The synthesis of the Mannich base N,N’-bis(antipyryl-4-methyl)-piperazine (BAMP) (1), its crystal structure as well as the synthesis and the crystal structure of the copper complex Cu(BAMP)(ClO4)2 (2) are reported. C28H34N6O2 ∙ 4H2O (BAMP ∙ 4H2O) crystallizes with triclinic symmetry, space group P1̄, lattice parameters: a = 704,9(2), b = 983,4(2), c = 1198,9(3) pm, α = 68,72°, β = 73,62°, γ = 78,49°. The copper-complex Cu(BAMP)(ClO4)2 crystallizes with tetragonal symmetry, space group P42/n, lattice parameters: a = 2295,1(3), c = 1412,2(2) pm. The copper(II) atom is five-coordinate by the two nitrogen atoms belonging to the piperazine ring and the oxygen atoms of the antipyrinemoieties. The geometry of the copper(II) atom can be described as a square-based pyramid with the N2O2 donor atoms of BAMP forming the basal plane and an oxygen atom of the neighbouring complex molecule occupying the apical position. BAMP acts as a tetradentate ligand, which incorporates a piperazine-fused ring. The structural parameters illustrate well the reinforcing effect exerted by the double “straps” of the piperazine molecule.
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46

Valenta, Vladimír, Zdeněk Prošek, Jiřina Metyšová, Martin Valchář, Antonín Dlabač, and Miroslav Protiva. "Cataleptic and noncataleptic neuroleptic agents: Synthesis and pharmacology of 4-(2-chloro and 8-chloro substituted 10,11-dihydrodibenzo[b,f]thiepin-10-yl)piperazine-1-ylalkyl ethers and sulfides." Collection of Czechoslovak Chemical Communications 50, no. 5 (1985): 1070–77. http://dx.doi.org/10.1135/cccc19851070.

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The title compounds Iab-Viab were prepared by substitution reactions of 2,11-dichloro- and 2,10-dichloro-10,11-dihydrodibenzo[b,f]thiepin with 1-(2-methoxyethyl)piperazine, 1-(3-methoxypropyl)piperazine, 1-(2-ethoxyethyl)piperazine, 1-(2-phenoxyethyl)piperazine, 1-(2-methylthioethyl)piperazine and 1-(2-phenylthioethyl)piperazine; they were transformed to hydrochlorides, maleates or methanesulfonates. Compounds of series a (8-chloro derivatives) are neuroleptics, with relatively strong cataleptic, antiapomorphine and central depressant activities (Ia, IIa, IIIa,Va) unless the volume and lipophilicity of the N-substituent exceeds certain limits (IVa and VIa are almost nontoxic and little active). Compounds of series b (2-chloro derivatives) are noncataleptic and devoid of the antiapomorphine potency; only two of them (IIb, Vb), however, showed a more pronounced effect in the test of influencing the turnover and metabolism of dopamine in the rat brain striatum.
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47

Chen, Jinhong, Junfang Li, Longqing Zhu, Xue Peng, Yiyue Feng, Yingmei Lu, Xiaoling Hu, Jianpin Liang, Quanyi Zhao, and Zhen Wang. "Total synthesis and structure revision of chrysamide B." Organic Chemistry Frontiers 5, no. 23 (2018): 3402–5. http://dx.doi.org/10.1039/c8qo00949j.

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48

Jílek, Jiří, Jiří Holubek, Emil Svátek, Jiřina Metyšová, Josef Pomykáček, Zdeněk Šedivý, and Miroslav Protiva. "Potential metabolites of the neuroleptic agents belonging to the 8-methylthio-10-piperazino-10,11-dihydrodibenzo[b,f]thiepin series; Synthesis of 2-hydroxy and 3-hydroxy derivatives." Collection of Czechoslovak Chemical Communications 50, no. 10 (1985): 2179–90. http://dx.doi.org/10.1135/cccc19852179.

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The acid VI, prepared by reaction of potassium salts of (2-iodo-5-methoxyphenyl)acetic acid and 4-(methylthio)thiophenol in the presence of copper, was transformed via intermediates VII-IX to 2-methoxy-8-methylthio-10-piperazino-10,11-dihydrodibenzo[b,f]thiepins X and XI. Their demethylation with boron tribromide afforded 2-hydroxy derivatives of the neuroleptic agents methiothepin and oxyprothepin I and II. 11-Chloro-7-methoxy-2-methylthio-10,11-dihydrodibenzo[b,f]thiepin was subjected to substitution reactions with 1-methylpiperazine and 1-(ethoxycarbonyl)piperazine and gave piperazine derivatives XIII and XIV, out of which the latter gave the secondary amine XV by alkaline hydrolysis. The ethers XIII and XV were also cleaved with boron tribromide and gave 3-hydroxy derivatives of methiothepin (III) and its demethyl derivative IV. The phenols I, II, and IV are potential metabolites of the mentioned neuroleptic agents; compound III, which already was identified as a metabolite, disclosed properties of a strong and cataleptic neuroleptic agent with prolonged duration of the effects. The methoxy compounds X, XI, and XIII are practically devoid of the neuroleptic activity.
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49

Chen, Mingwei, Jinyu Hu, Xiaoli Tang, and Qiming Zhu. "Piperazine as an Inexpensive and Efficient Ligand for Pd-Catalyzed Homocoupling Reactions to Synthesize Bipyridines and Their Analogues." Current Organic Synthesis 16, no. 1 (February 4, 2019): 173–80. http://dx.doi.org/10.2174/1570179415666180913131905.

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Aim and Objective: The synthesis of bipyridines, especially 2, 2’-bipyridines, remains challenging because the catalytic cycle can be inhibited due to coordination of bipyridine to transition metal. Thus, the development of efficient methods for the synthesis of bipyridines is highly desirable. In the present work, we presented a promising approach for preparation of bipyridines via a Pd-catalyzed reductive homocoupling reaction with simple piperazine as a ligand. Materials and Methods: Simple and inexpensive piperazine was used as a ligand for Pd-catalyzed homocoupling reaction. The combination of Pd(OAc)2 and piperazine in dimethylformamide (DMF) was observed to form an excellent catalyst and efficiently catalyzed the homocoupling of azaarenyl halides, in which DMF was used as the solvent without excess reductants although stoichiometric reductant was generally required to generate the low-oxidation-state active metal species in the catalytic cycles. </P><P> Results: In this case, good to excellent yields of bipyridines and their (hetero) aromatic analogues were obtained in the presence of 2.5 mol% of Pd(OAc)2 and 5 mol% of piperazine, using K3PO4 as a base in DMF at 140°C. Conclusion: According to the results, piperazine as an inexpensive and efficient ligand was used in the Pd(OAc)2-catalyzed homocoupling reaction of heteroaryl and aryl halides. The coupling reaction was operationally simple and displayed good substrate compatibility.
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Kottakki, Naveen K., and Amperayani K. Rao. "SYNTHESIS OF PIPERINE - PIPERAZINE ANALOGUES AND THEIR ANTIBACTERIAL ACTIVITY." INDIAN DRUGS 58, no. 06 (August 17, 2021): 30–35. http://dx.doi.org/10.53879/id.58.06.12311.

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In the current study, a series of piperine – piperazine analogues (5a to 5f) were designed and synthesized. The piperine was isolated from pepper and used for the conjugation with heterocyclic moiety for better biological activity. The piperazine heterocyclic was chosen for conjugation with piperine. The newly synthesized structures were determined by IR, 1H NMR and 13C NMR spectral data. The compounds were examined for their anti‐microbial activity against gram-positive (Bacillus subtilis) and gram-negative (Vibrio cholerae) bacteria using the agar well diffusion method. The newly synthesized compounds exhibited capable activities against V. cholerae and B. subtilis and it showed minimum inhibitory concentration. Among all the synthesized compounds, 5f has the highest activity (26 mm) against gram-positive bacteria and (29mm) against gram-negative bacteria. The remaining compounds showed appreciable antibacterial activity. The enhanced activity of the synthesized compounds may be due to the presence of conjugated amide linkage with the natural product piperine and piperazine heterocyclic molecule. The substituents present on the aromatic (nitro-substituted) ring also influenced the activity of the compound.
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