Relevant bibliographies by topics / Route scouting

Contents

  1. Journal articles
  2. Dissertations / Theses
  3. Book chapters
  4. Conference papers

Academic literature on the topic 'Route scouting'

Author: Grafiati
Published: 9 March 2023
Last updated: 10 March 2023

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Journal articles on the topic "Route scouting"

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Chapuis, Christian, Eric Walther, Fabrice Robvieux, Claude-Alain Richard, Laurent Goumaz, and Jean-Yves de Saint Laumer. "Route Scouting towards a Methyl Jasmonate Precursor." Helvetica Chimica Acta 99, no. 2 (February 2016): 95–109. http://dx.doi.org/10.1002/hlca.201500257.

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Dahl, Allan C., Michael J. Mealy, Martin A. Nielsen, Lars O. Lyngsø, and Cristina Suteu. "Route Scouting and Process Development of Lu AA26778." Organic Process Research & Development 12, no. 3 (May 2008): 429–41. http://dx.doi.org/10.1021/op7002584.

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Pierre, Romain, Anne Brethon, Sylvain A. Jacques, Aurélie Blond, Sandrine Chambon, Sandrine Talano, Catherine Raffin, et al. "Novel library synthesis of 3,4-disubstituted pyridin-2(1H)-ones via cleavage of pyridine-2-oxy-7-azabenzotriazole ethers under ionic hydrogenation conditions at room temperature." Beilstein Journal of Organic Chemistry 17 (January 18, 2021): 156–65. http://dx.doi.org/10.3762/bjoc.17.16.

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In our hands, efficient access to the 4-amino-3-carboxamide disubstituted pyridine-2(1H)-one kinase hinge-binder motif proved to be more challenging than anticipated requiring a significant investment in route scouting and optimization. This full paper focuses on the synthesis issues that we encountered during our route exploration and the original solutions we found that helped us to identify two optimized library-style processes to prepare our large kinase inhibitor library.
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Lafitte, Guillaume, Veronique Parnet, Romain Pierre, Catherine Raffin, Rodolphe Vatinel, Branislav Musicki, Loic Tomas, et al. "Route scouting and optimization of a potent sulfoximine-based inverse agonist of RORγt." Tetrahedron 74, no. 40 (October 2018): 5974–86. http://dx.doi.org/10.1016/j.tet.2018.08.043.

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Lane, Jonathan W., Keith L. Spencer, Sagar R. Shakya, Nicholas C. Kallan, Peter J. Stengel, and Travis Remarchuk. "Synthesis of Akt Inhibitor Ipatasertib. Part 1. Route Scouting and Early Process Development of a Challenging Cyclopentylpyrimidine Intermediate." Organic Process Research & Development 18, no. 12 (November 19, 2014): 1641–51. http://dx.doi.org/10.1021/op500271w.

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Buitrago Santanilla, Alexander, Erik L. Regalado, Tony Pereira, Michael Shevlin, Kevin Bateman, Louis-Charles Campeau, Jonathan Schneeweis, et al. "Nanomole-scale high-throughput chemistry for the synthesis of complex molecules." Science 347, no. 6217 (November 20, 2014): 49–53. http://dx.doi.org/10.1126/science.1259203.

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At the forefront of new synthetic endeavors, such as drug discovery or natural product synthesis, large quantities of material are rarely available and timelines are tight. A miniaturized automation platform enabling high-throughput experimentation for synthetic route scouting to identify conditions for preparative reaction scale-up would be a transformative advance. Because automated, miniaturized chemistry is difficult to carry out in the presence of solids or volatile organic solvents, most of the synthetic “toolkit” cannot be readily miniaturized. Using palladium-catalyzed cross-coupling reactions as a test case, we developed automation-friendly reactions to run in dimethyl sulfoxide at room temperature. This advance enabled us to couple the robotics used in biotechnology with emerging mass spectrometry–based high-throughput analysis techniques. More than 1500 chemistry experiments were carried out in less than a day, using as little as 0.02 milligrams of material per reaction.
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Hardegger, Leo A., Franck Mallet, Barbara Bianchi, Chunlong Cai, Alexandre Grand-Guillaume Perrenoud, Roger Humair, Richard Kaehny, et al. "Toward a Scalable Synthesis and Process for EMA401, Part I: Late Stage Process Development, Route Scouting, and ICH M7 Assessment." Organic Process Research & Development 24, no. 9 (August 20, 2020): 1743–55. http://dx.doi.org/10.1021/acs.oprd.0c00215.

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Kleiner, Yolanda, Armin Bauer, Peter Hammann, Sören M. M. Schuler, and Christoph Pöverlein. "Total Synthesis of Floyocidin B: 4,5-Regioselective Functionalization of 2-Chloropyridines." Chemistry 5, no. 1 (January 16, 2023): 168–78. http://dx.doi.org/10.3390/chemistry5010014.

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The recently discovered natural product (NP) (+)-floyocidin B with antimicrobial activity against Mycobacterium tuberculosis displays a hitherto unknown dihydroisoquinolinone scaffold in the class of the epoxyquinone NPs. The 4,5-regioselective functionalization of 2-chloropyridines was identified as a suitable strategy leading to the total syntheses of (+)-floyocidin B and analogs. In this paper, we present the long and winding evolution process to the final synthetic pathway, including model systems for route scouting and elucidation of side products, which enabled us to understand the unique reactivity of this unprecedented scaffold. A special focus was laid on method studies with different 2-chloropyridines, disclosing an unexpected effect of the 2-chloro substituent on the regioselectivity compared to 2-unsubstituted or carbon-substituted pyridines. Finally, a head-to-head comparison with the previously described synthesis of all four stereoisomers of the NP (−)-avicennone C revealed significant differences in the reactivity of these structurally closely related scaffolds.
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Folsom, Larkin, Masahiro Ono, Kyohei Otsu, and Hyoshin Park. "Scalable information-theoretic path planning for a rover-helicopter team in uncertain environments." International Journal of Advanced Robotic Systems 18, no. 2 (March 1, 2021): 172988142199958. http://dx.doi.org/10.1177/1729881421999587.

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Mission-critical exploration of uncertain environments requires reliable and robust mechanisms for achieving information gain. Typical measures of information gain such as Shannon entropy and KL divergence are unable to distinguish between different bimodal probability distributions or introduce bias toward one mode of a bimodal probability distribution. The use of a standard deviation (SD) metric reduces bias while retaining the ability to distinguish between higher and lower risk distributions. Areas of high SD can be safely explored through observation with an autonomous Mars Helicopter allowing safer and faster path plans for ground-based rovers. First, this study presents a single-agent information-theoretic utility-based path planning method for a highly correlated uncertain environment. Then, an information-theoretic two-stage multiagent rapidly exploring random tree framework is presented, which guides Mars helicopter through regions of high SD to reduce uncertainty for the rover. In a Monte Carlo simulation, we compare our information-theoretic framework with a rover-only approach and a naive approach, in which the helicopter scouts ahead of the rover along its planned path. Finally, the model is demonstrated in a case study on the Jezero region of Mars. Results show that the information-theoretic helicopter improves the travel time for the rover on average when compared with the rover alone or with the helicopter scouting ahead along the rover’s initially planned route.
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Schäfer, Gabriel, Tony Fleischer, Nicole Blumer, Megan Udry, Stefan Reber, Ian Stansfield, Yuanhua Liu, Yan Li, and Pixu Li. "Initial Route Scouting and Final Process Development for the Multi-Kg Production of 3-Fluoro-6-methoxyquinoline from p-Anisidine and 2-Fluoromalonic Acid." Organic Process Research & Development 26, no. 2 (January 20, 2022): 347–57. http://dx.doi.org/10.1021/acs.oprd.1c00414.

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Dissertations / Theses on the topic "Route scouting"

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Chiossi, Francesco. "Sviluppo di un processo in continuo per la sintesi di un intermedio farmaceutico." Master's thesis, Alma Mater Studiorum - Università di Bologna, 2022. http://amslaurea.unibo.it/25476/.

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In this work process for the coupling reaction between a secondary chiral alcohol and a heterocyclic amine is studied. The chiral configuration must be inverted. The mesylate derivative of the alcohol is known to be unstable, so a continuous process with no isolation is developed for alcohol activation and amine coupling. This approach led to poor results in terms of yield and chiral purity. As an alternative approach, the Mitsunobu reaction is used. The application of flow chemistry to this reaction is promising since it uses highly energetic compounds and has a fast kinetic. Despite these premises, this approach led to worst results in yield and selectivity when using the substrate of interest. The reaction kinetic basically addresses selectivity towards by-products that in this case are reduced by mass transfer limitation. Mass transfer is the rate determining step.
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Calogero, F. "NEW SYNTHETIC PROCESSES FOR THE APIS INDUSTRIAL PRODUCTION: THE CASE OF SILODOSIN." Doctoral thesis, Università degli Studi di Milano, 2014. http://hdl.handle.net/2434/243613.

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This thesis is focused on the development of new synthetic processes for the production of already known Active Pharmaceutical Ingredients (APIs). The research work was performed in the laboratories of Dipharma Francis srl, a company which operates in the generic drug market. The launch of the generic version of a drug in the market often leads to lowering of product prices for both the branded product and the generic ones. For this reason, the process adopted to produce an API has to be innovative, efficient, safe and, of course, cheaper than the existing ones, in order to be competitive in the market. During my Ph.D. I worked on the synthesis of some APIs, in particular here I report the feasibility and development studies of an alternative process to produce silodosin. Silodosin is an API used as a treatment for the symptoms of Benign Prostatic Hyperplasia (BPH). In order to establish the synthetic strategy and to outline our freedom to operate, an accurate survey of the whole patent literature about silodosin has been done. During the feasibility study several synthetic approaches have been tried in order to functionalise indoline at positions 5 and 7. A copper(I) catalysed C-arylation reaction and a regioselective electrophilic aromatic substitution revealed to be the best choices to introduce respectively substituents in position 5 and 7 of indoline. The synthesis continued with a diastereoselective reductive amination which after crystallisation yielded optically pure amine intermediate that is the key intermediate for the synthesis of silodosin and ended converting amine intermediate into Silodosin using already reported procedures. Our new process to prepare silodosin starting from commercially available and cheap indoline consists of 11 steps. The whole synthetic route has been performed in gram scale using only 4 purifications of key intermediates. Silodosin has been finally obtained in a 10% overall yield, with a purity greater than 99% measured by HPLC and an optical purity greater than 99% measured by HPLC on chiral stationary phase.
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Book chapters on the topic "Route scouting"

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Safaei, F., A. Khonsari, M. Fathy, N. Talebanfard, and M. Ould-Khaoua. "Communication–Prediction of Scouting Switching in Adaptively-Routed Torus Networks." In Lecture Notes in Computer Science, 466–75. Berlin, Heidelberg: Springer Berlin Heidelberg, 2007. http://dx.doi.org/10.1007/978-3-540-74784-0_47.

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Conference papers on the topic "Route scouting"

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Zebardast, Mohammad, and Farshad Safaei. "Stochastic modeling of Scouting Switching for adaptively-routed mesh networks." In 2011 9th IEEE/ACS International Conference on Computer Systems and Applications (AICCSA). IEEE, 2011. http://dx.doi.org/10.1109/aiccsa.2011.6126583.

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Carey, Drew A., Daniel F. Doolittle, and Kevin Smith. "Forward Scouting: Use of Sediment Profile Imagery in Conjunction with Multibeam Echosounder Mapping for Offshore Wind Cable Routes and Site Characterization." In Offshore Technology Conference. Offshore Technology Conference, 2019. http://dx.doi.org/10.4043/29220-ms.

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