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An Unexpected Incident during the Manufacture of O-(Diphenylphosphinyl)hydroxylamine Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-09-28 Curtis J. Rieder, Mark V. Smith
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Optimization and Development of a Scalable Palladium-Catalyzed C–H Activation Process for the Geometry-Selective Preparation of Kilograms of YLF466D, a Potent AMP-Activated Protein Kinase Activator Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-09-27 Jianpeng Yin, Desheng Zhan, Hui Ma, Huanan Liu, Lifang Yu, Yangming Zhang, Fajun Nan
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Directed Ortho Metalation in 2021: A Tribute to Victor Snieckus (August 1, 1937–December 18, 2020) Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-09-24 Paul Knochel, Kevin P. Cole
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Monte Carlo Analysis-Based CapEx Uncertainty Estimation of New Technologies: The Case of Photochemical Lamps Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-09-20 Levente L. Simon, Michael Dieckmann, Alan Robinson, Thomas Vent-Schmidt, Dominique Marantelli, Ralf Kohlbrenner, Alexandre Saint-Dizier, Denis Gribkov, Jean-Philippe Krieger
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Development and Scale-Up of a Novel Photochemical C–N Oxidative Coupling Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-09-17 Alan Robinson, Michael Dieckmann, Jean-Philippe Krieger, Thomas Vent-Schmidt, Dominique Marantelli, Ralf Kohlbrenner, Denis Gribkov, Levente L. Simon, David Austrup, Alexandre Rod, Christian G. Bochet
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Review of Synthetic Routes and Crystalline Forms of the Oncology Drugs Capmatinib, Selpercatinib, and Pralsetinib Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-09-17 David L. Hughes
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Some Items of Interest to Process R&D Chemists and Engineers Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-09-08 Paul F. Richardson, Alan Steven, Robert B. Kargbo, Carlos Mateos, Andrei A. Zlota, Christopher C. Nawrat, Kiran Matcha, Antonio Ramirez, John Knight
This article has not yet been cited by other publications.
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A Journey toward the Syntheses of γ-Amino-β-hydroxybutyric Acid (GABOB) and Carnitine Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-08-18 Krishnaji Tadiparthi, Pragya Anand
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Fully Continuous Flow Synthesis of 3-Chloro-4-oxopentyl Acetate: An Important Intermediate for Vitamin B1 Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-08-27 Meifen Jiang, Minjie Liu, Chao Yu, Dang Cheng, Fener Chen
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Extended Solution-phase Peptide Synthesis Strategy Using Isostearyl-Mixed Anhydride Coupling and a New C-Terminal Silyl Ester-Protecting Group for N-Methylated Cyclic Peptide Production Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-08-23 Akihiro Nagaya, Shota Murase, Yuji Mimori, Kazuya Wakui, Madoka Yoshino, Ayumu Matsuda, Yutaka Kobayashi, Haruaki Kurasaki, Douglas R. Cary, Keiichi Masuya, Michiharu Handa, Naoki Nishizawa
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In-line Monitoring of Microgel Synthesis: Flow versus Batch Reactor Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-08-18 Luise F. Kaven, Hanna J. M. Wolff, Lukas Wille, Matthias Wessling, Alexander Mitsos, Joern Viell
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Integrated Multistep Photochemical and Thermal Continuous Flow Reactions: Production of Bicyclic Lactones with Kilogram Productivity Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-09-08 Rowena A. Howie, Luke D. Elliott, Surajit Kayal, Xue-Zhong Sun, Magnus W. D. Hanson-Heine, Jonathan Hunter, Charlotte A. Clark, Ashley Love, Christopher Wiseall, Darren S. Lee, Martyn Poliakoff, Kevin I. Booker Milburn, Michael W. George
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Effective Phosphorylation of 2,2′-Methylene-bis(4,6-di-tert-butyl) Phenol in Continuous Flow Reactors Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-08-23 Hanlin Yao, Li Wan, Xiaoyu Zhao, Yahui Guo, Jian Zhou, Xiaofan Bo, Yuxin Mao, Zhong Xin
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Continuous Synthesis and Separation of p-Bromobenzyl Bromide Using Atom-Efficient Bromination of p-Bromotoluene without Any Organic Effluent: Potential for Green Industrial Practice Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-08-25 Sonam V. Sancheti, Ganapati D. Yadav
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Efficient Synthesis of a Key Intermediate for Baloxavir Marboxil from a Greener Starting Material: Ethylene Glycol Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-09-08 Zhongqing Wang, Zihong Zhou, Jingping Kou, Shuming Wu, Yongbo Xu, Jiebin Zeng
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DMF-Assisted Iodination Side Reaction during the Preparation of Disulfide Peptides, Its Substrate/Solvent/pH Dependence, and Implications on Disulfide-Peptide Production Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-08-25 Yi Yang, Lena Hansen, Aleksandra Fraczek, Fabrizio Badalassi, Johan Kjellström
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Continuous and Selective Hydrogenation of Heterocyclic Nitroaromatics in a Micropacked Bed Reactor Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-08-15 Xiaonan Duan, Xuepeng Wang, Xingkun Chen, Jisong Zhang
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Experiment and Simulations for the Thermal Safety of the Nitration Reaction Liquid of the Final State in the Synthesis Process of N-Nitrodihydroxyethyl Dinitrate (DINA) Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-08-31 Yanlong Zhu, Jing An, Jing Zhou, Xiaofeng Wang, Hai Chang, Li Ding
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Investigation of Wet Milling and Indirect Ultrasound as Means for Controlling Nucleation in the Continuous Crystallization of an Active Pharmaceutical Ingredient Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-09-01 Yihui Yang, Bilal Ahmed, Christopher Mitchell, Justin L. Quon, Humera Siddique, Ian Houson, Alastair J. Florence, Charles D. Papageorgiou
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Kinetics and Hazards of 4-Vinylbenzyl Chloride Storage and Thermal Decomposition of Di-4-methylbenzoyl Peroxide by DSC and TAM Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-08-24 Soham Dutta, Florin Dan, Steven Horsch
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Scale-Up of a Continuous Manufacturing Process of Edaravone Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-08-27 Shuhao Zhou, Qingxia Hong, Wenliu Mei, Yan He, Chengjun Wu, Tiemin Sun
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Crystallization-Based Synthetic Route to Antimalarial Agent BRD5018: Diazocene Ring Formation via a Staudinger-aza-Wittig Reaction on an Azetidine-Ribose Template Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-09-15 Branko Mitasev, Jiong Yang, Fabian Gusovsky, Dixit Girish, Anil Shahaji Khile, Venkata Sasidhar Balla, Venugopalarao Vikram, Anand Vaddi, Srikanth Bathula, Srinivasa Rao Sugandham, Chiranjeevi Terli, Vijay Kalla, Pavan Kumar Rayaprolu, Ravi Kumar Talabhakthula, Masaharu Gotoda, Bruno Melillo, Stuart L. Schreiber, Francis G. Fang
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Scalable Synthesis of β-Lactamase Inhibitor QPX7728 by Sequential Nickel-Catalyzed Boron Insertion into a Benzofuran Substrate and Enantioselective Cyclopropanation of the Resulting Vinylboronate Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-09-15 Serge H. Boyer, Angela Gonzalez-de-Castro, J.A. Hubertus Dielemans, Laurent Lefort, Zuolin Zhu, Matthias Gnahn, Julia Schörghuber, Stefan Steinhofer, André H. M. de Vries, Scott J. Hecker
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Consolidating and Managing Data for Drug Development within a Pharmaceutical Laboratory: Comparing the Mapping and Reporting Tools from Software Applications Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-09-14 Arvin Moser, Alexander E. Waked, Joseph DiMartino
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Development of a Practical Manufacturing Process to Relebactam via Thorough Understanding of the Origin and Control of Oligomeric Impurities Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-09-13 Jungchul Kim, Tetsuji Itoh, Feng Xu, Zachary E. X. Dance, Jacob H. Waldman, Debra J. Wallace, Feiyue Wu, Roman Kats-Kagan, Anil R. Ekkati, Andrew P. J. Brunskill, Feng Peng, Patrick S. Fier, Jennifer V. Obligacion, Benjamin D. Sherry, Zhijian Liu, Khateeta M. Emerson
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Accelerated Development of a Scalable Synthesis of CY6463, a CNS-Penetrant sGC Stimulator for the Treatment of Neurodegenerative Diseases Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-09-13 Debra J. Wallace, Thomas Storz, Anna Balanov, William S. Kissel
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An Efficient Second-Generation Manufacturing Process for the pan-RAF Inhibitor Belvarafenib Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-09-10 Daniel Zell, Michael E. Dalziel, Diane E. Carrera, Andreas Stumpf, Stephan Bachmann, Eduardo Mercado-Marin, Stefan G. Koenig, Haiming Zhang, Francis Gosselin
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Complexation of Polyethyleneglycol Containing Small Molecules with Magnesium Chloride as a Purification and Isolation Strategy Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-09-10 Bin Zheng, Jun Li, Charles Pathirana, Shenjie Qiu, Michael A. Schmidt, Martin D. Eastgate
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Predicting the Fire and Explosion Properties of Early-Phase Active Pharmaceutical Ingredients Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-09-10 Antony Janes, Roy C. Flanagan, Andrew Payne, Chris Newlands
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Identification and Screening of Potential Organic Solvents for the Liquid–Liquid Extraction of Aromatics Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-09-09 Nivaar Brijmohan, Kuveneshan Moodley, Caleb Narasigadu
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Practical Gas Cylinder-Free Preparations of Important Transition Metal-Based Precatalysts Requiring Gaseous Reagents Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-09-09 Hongwei Sun, Alexander Ahrens, Steffan K. Kristensen, Laurynas Gausas, Bjarke S. Donslund, Troels Skrydstrup
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Synthesis of Fingolimod Employing Regioselective Aziridine Ring-Opening Reaction as a Key Step Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-09-03 Jan Doubský, Stanislav Rádl, Josef Cinibulk, Robert Klvaňa
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Application of Biocatalytic Reductive Amination for the Synthesis of a Key Intermediate to a CDK 2/4/6 Inhibitor Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-09-03 Shengquan Duan, Daniel W. Widlicka, Michael P. Burns, Rajesh Kumar, Ian Hotham, Jean-Nicolas Desrosiers, Paul Bowles, Kris N. Jones, Lindsay D. Nicholson, Michele T. Buetti-Weekly, Lu Han, Jeremy Steflik, Eric Hansen, Cheryl M. Hayward, Holly Strohmeyer, Sébastien Monfette, Scott C. Sutton, Christopher Morris
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Synthetic and Chromatographic Challenges and Strategies for Multigram Manufacture of KRASG12C Inhibitors Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-08-24 Grigorios Nikitidis, Anna-Carin C. Carlsson, Staffan Karlsson, Andrew D. Campbell, Calum Cook, Kuangchu Dai, Hans Emtenäs, Anna C. Jonson, Hanna Leek, Marcus Malmgren, Štefan Moravčík, Subhash Pithani, Matthew R. Tatton, Hucheng Zhao, Kristina Öhlén
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Some Items of Interest to Process R&D Chemists and Engineers Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-08-09 Sylvain Guizzetti, James A. Schwindeman, David S. B. Daniels, James J. Douglas, Alex Kosanovich, James P. Phelan, Wenyi Zhao, Sylvain Petit, Christopher B. Kelly, John Knight
This article has not yet been cited by other publications.
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Regulatory Highlights Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-07-21 Andrew Teasdale, Michael W. Urquhart
It is almost inevitable that any regulatory highlights review at present will be dominated by N-nitrosamines. Therefore, “where are we?” and “what next?” are key questions that we explore within this review.
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Organosilanes in Metal-Catalyzed, Enantioselective Reductions Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-07-26 Gerald L. Larson, Richard J. Liberatore
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Nitrosamine Reactivity: A Survey of Reactions and Purge Processes Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-07-18 Christopher J. Borths, Michael Burns, Timothy Curran, Nathan D. Ide
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Recent Advances in Nonprecious Metal Catalysis Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-08-10 Robert A. Singer, Sebastien Monfette, David Bernhardson, Sergei Tcyrulnikov, Aran K. Hubbell, Eric C. Hansen
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An Easy, Convenient, and Safe Process for the Synthesis of Lofexidine Hydrochloride Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-07-27 Monica Donnola, Annalisa Airoldi, Alessandro Barozza, Jacopo Roletto, Paolo Paissoni
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Toward a Practical, Two-Step Process for Molnupiravir: Direct Hydroxamination of Cytidine Followed by Selective Esterification Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-07-28 Dinesh J. Paymode, N. Vasudevan, Saeed Ahmad, Appasaheb L. Kadam, Flavio S.P. Cardoso, Justina M. Burns, Daniel W. Cook, Rodger W. Stringham, David R. Snead
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Improved Multigram Route to a Tricyclic Key Intermediate for Dibenzosuberone-Based p38 Inhibitors via an Optimized Early-Stage Heck Coupling Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-08-04 Michael Forster, Heike K. Wentsch-Teltschik, Stefan A. Laufer
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New Scalable Synthetic Routes to ELQ-300, ELQ-316, and Other Antiparasitic Quinolones Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-08-04 Sovitj Pou, Rozalia A. Dodean, Lisa Frueh, Katherine M. Liebman, Rory T. Gallagher, Haihong Jin, Robert T. Jacobs, Aaron Nilsen, David R. Stuart, J. Stone Doggett, Michael K. Riscoe, Rolf W. Winter
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Proof-of-Concept Design of an In-Line pH Neutralization System with Coarse and Fine Adjustments for the Continuous Manufacturing of Pharmaceuticals Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-08-05 Ke Wen, Chuntian Hu, Wei Wu, Khrystyna Shvedova, Stephen C. Born, Bayan Takizawa, Salvatore Mascia
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Practical Estimation Techniques for Determination of Reaction Heat Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-07-26 Min Sheng
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Multigram Synthesis of Trioxanes Enabled by a Supercritical CO2 Integrated Flow Process Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-06-25 Lingqiao Wu, Bruna L. Abreu, Alexander J. Blake, Laurence J. Taylor, William Lewis, Stephen P. Argent, Martyn Poliakoff, Hamza Boufroura, Michael W. George
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Development of a Safe Continuous Process to Sodium Nitrotetrazolate via Solid Phase “Catch and Release” Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-07-14 Robert H. Muir, Jon Bragg, Andrew Pearsall, Matthew Jorgensen, Brittany Sims, Kyle Yonoski, Neha Mehta, Jerry S. Salan
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Development and Scale-Up of an Asymmetric Synthesis of AZD8186 Using the Fukuyama Modification of the Mitsunobu Reaction Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-07-15 Peter R. Moore, James C. Muir, Jerome Dubiez, Kevin W. Leslie, Paula Tomlin, Marc McCormick, Sophie L. Janbon, Philip Cornwall, Per Ryberg, Robert Berg
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Six-Step Gram-Scale Synthesis of the Human Immunodeficiency Virus Integrase Inhibitor Dolutegravir Sodium Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-07-12 Jule-Philipp Dietz, Tobias Lucas, Jonathan Groß, Sebastian Seitel, Jan Brauer, Dorota Ferenc, B. Frank Gupton, Till Opatz
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Copper-Catalyzed, Aerobic Oxidation of Hydrazone in a Three-Phase Packed Bed Reactor Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-07-22 Taylor A. Hatridge, Bo Wei, Huw M. L. Davies, Christopher W. Jones
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Impurity Dimethylcarbamoyl-OBt Detected in an API Induced by the Degradation of HBTU in DMF Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-07-27 Yi Yang, Lena Hansen, Jörgen Kjellgren Sjögren, Ileana Rodríguez León, Jean-Marie Receveur, Fabrizio Badalassi
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Thermal Hazards of Using Propargyl Alcohol with Strong Bases Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-07-28 Derek B. Brown, Ayman D. Allian, Ying Chen
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A Holistic Strategy for Cyanide Control and Safety for Pharmaceutical Manufacturing Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-08-09 Michael A. Zompa, Michael J. Di Maso, Francisco Guzman, Ralph Zhao, Lisa Jellett, Rebecca Arvary, Siqing Song, Darryl Chang, Hong Ren, Sachin Lohani
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Daisy-Chaining Photo- and Thermal Chemistry: Multistep Continuous Flow Synthesis of Visible-Light-Mediated Photochemistry with a High-Temperature Cascade Reaction Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-07-19 Luke D. Elliott, Kevin I. Booker-Milburn, Alastair J. J. Lennox
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Practical Synthesis of (+)-Biotin Key Intermediate by Calcium Borohydride Reduction and Temperature-Dependent Purity Upgrade during Crystallization Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-07-16 Masahiko Seki, Yusuke Takahashi
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Insights into Fast Amide Couplings in Aqueous Nanomicelles Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-07-08 Sudripet Sharma, Gaganpreet Kaur, Sachin Handa
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Synthesis of Enantiopure Unnatural Amino Acids by Metallaphotoredox Catalysis Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-07-26 Tomer M. Faraggi, Caroline Rouget-Virbel, Juan A. Rincón, Mario Barberis, Carlos Mateos, Susana García-Cerrada, Javier Agejas, Oscar de Frutos, David W. C. MacMillan
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Finkelstein Reaction in Non-polar Organic Solvents: A Streamlined Synthesis of Organic Iodides Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-08-02 Yusuke Takahashi, Masahiko Seki
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Safety Assessments Supporting Scale-up of Chemistry Involving Hydrogen Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-08-11 Cuixian Yang, Tao Wang, Daniel J. Muzzio, Stephen Van Cleaf, Eric M. Phillips, Adam J. Fine, Thomas P. Vickery, Alexei Kalinin, Stephen M. Dalby, Theodore R. Furman, Ryan Flessner, Analisse Rosario, Ralph Zhao, Megan Roth
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Catalytic Static Mixer-Enabled Hydrogenation of a Key Fenebrutinib Intermediate: Real-Time Analysis for a Stable and Scalable Process Org. Process Res. Dev. (IF 3.317) Pub Date : 2021-07-28 René Lebl, Stephan Bachmann, Paolo Tosatti, Joerg Sedelmeier, Kurt Püntener, Jason D. Williams, C. Oliver Kappe
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