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Predicting Performance of Photochemical Transformations for Scaling Up in Different Platforms by Combining High-Throughput Experimentation with Computational Modeling Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-09-03 Melda Sezen-Edmonds; Jose E. Tabora; Benjamin M. Cohen; Serge Zaretsky; Eric M. Simmons; Trevor C. Sherwood; Antonio Ramirez
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Taming Troublesome Suzuki–Miyaura Reactions in Water Solution of Surfactants by the Use of Lecithin: A Step beyond the Micellar Model Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-09-04 Chiara Ceriani; Erika Ghiglietti; Mauro Sassi; Sara Mattiello; Luca Beverina
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Effective Control of Crystal Size via an Integrated Crystallization, Wet Milling, and Annealing Recirculation System Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-08-26 Wei Meng; Eric Sirota; Hanzhou Feng; Jonathan P. McMullen; Lorenzo Codan; Aaron S. Cote
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Renewable Solvents for Palladium-Catalyzed Carbonylation Reactions Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-09-04 Aya Ismael; Ashot Gevorgyan; Troels Skrydstrup; Annette Bayer
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Development of a Nitrene-Type Rearrangement for the Commercial Route of the JAK1 Inhibitor Abrocitinib Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-09-18 Christina G. Connor; Jacob C. DeForest; Phil Dietrich; Nga M. Do; Kevin M. Doyle; Shane Eisenbeis; Elizabeth Greenberg; Sarah H. Griffin; Brian P. Jones; Kris N. Jones; Michael Karmilowicz; Rajesh Kumar; Chad A. Lewis; Emma L. McInturff; J. Christopher McWilliams; Ruchi Mehta; Bao D. Nguyen; Anil M. Rane; Brian Samas; Barbara J. Sitter; Howard W. Ward; Mark E. Webster
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Some Items of Interest to Process R&D Chemists and Engineers Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-09-10 Paul Richardson; Alan Steven; Robert Kargbo; Christopher C. Nawrat; Carlos Mateos; Andrei A. Zlota; John Knight
Email addresses: [email protected]; [email protected]; [email protected]; [email protected]; [email protected]; [email protected]; [email protected]. This article has not yet been cited by other publications.
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Pathways for N-Nitroso Compound Formation: Secondary Amines and Beyond Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-07-28 Rocío López-Rodríguez; James A. McManus; Natasha S. Murphy; Martin A. Ott; Michael J. Burns
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Potential Safety Hazards Associated with Using N,N-Dimethylformamide in Chemical Reactions Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-08-06 Qiang Yang; Min Sheng; Yongliang Huang
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Development of a Scalable and Safer Synthesis of Diazeniumdiolates Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-08-11 Yong-Li Zhong; Daniel J. Muzzio; Mark Weisel; Li Zhang; Guy R. Humphrey; Kevin M. Maloney; Kevin R. Campos
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Large-Scale Practical Synthesis of Boc-Protected 4-Fluoro-l-Proline Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-08-07 Yasinalli Tamboli; Bharat Kashid; Ram Prasad Yadav; Mohammad Rafeeq; Arvind Y Merwade
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Study on Autocatalytic Decomposition of Dimethyl Sulfoxide (DMSO) Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-08-20 Yoshikuni Deguchi; Masafumi Kono; Yuto Koizumi; Yu-ichiro Izato; Atsumi Miyake
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Countercurrently Operated Reactive Extractor with an Additively Manufactured Enzyme Carrier Structure Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-08-03 Niclas Büscher; Claas Spille; John K. Kracht; Giovanni V. Sayoga; Ayad W. H. Dawood; Maria Isabelle Maiwald; Dirk Herzog; Michael Schlüter; Andreas Liese
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Potential for the Formation of N-Nitrosamines during the Manufacture of Active Pharmaceutical Ingredients: An Assessment of the Risk Posed by Trace Nitrite in Water Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-08-03 Ian W. Ashworth; Olivier Dirat; Andrew Teasdale; Matthew Whiting
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High-Throughput Screening of Reductive Amination Reactions Using Desorption Electrospray Ionization Mass Spectrometry Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-08-14 David L. Logsdon; Yangjie Li; Tiago Jose Paschoal Sobreira; Christina R. Ferreira; David H. Thompson; R. Graham Cooks
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Kinetics, Thermodynamics, and Scale-Up of an Azeotropic Drying Process: Mapping Rapid Phase Conversion with Process Analytical Technology Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-08-20 Zachary E. X. Dance; Morgan Crawford; Aaron Moment; Andrew Brunskill; Busolo Wabuyele
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Development of an Efficient Scale-Up Synthesis Method for a β3-Adrenergic Receptor Agonist, Ritobegron Ethyl Hydrochloride Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-07-31 Junichi Sonehara; Hidetoshi Isawa; Kiyoshi Kasai; Norihiko Kikuchi; Takehiro Ishikawa; Masahiro Kobayashi; Tetsuji Ozawa; Ritsu Suzuki; Makoto Kobayashi; Takayuki Ainai; Masayuki Nishimura; Yohei Saito; Kyoko Nakagawa-Goto
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Diethanolamine Boronic Esters: Development of a Simple and Standard Process for Boronic Ester Synthesis Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-08-04 Phillip A. Inglesby; Lauren R. Agnew; Holly L. Carter; Oliver T. Ring
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Practical Synthesis of a Stable Precursor for Positron Emission Tomography Imaging Agent 18F-GTP1 Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-07-28 Nicholas A. White; Kyle Clagg; Lauren E. Sirois; Ngiap-Kie Lim; William A. Nack; Paul D. O’Shea; Haiming Zhang; Francis Gosselin
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Development of a Practical, Biocatalytic Synthesis of tert-Butyl (R)-3-Hydroxyl-5-hexenoate: A Key Intermediate to the Statin Side Chain Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-08-21 Chen Hu; Minjie Liu; Xiaoping Yue; Zedu Huang; Fener Chen
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One-Pot Process for Synthesis of Nalbuphine Hydrochloride and Impurity Control Strategy Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-08-07 Tao Zhang; Zenong Wu; Yibo Chen; Weili Zhao; Zhezhou Yang; Fuli Zhang
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Development of Scalable Synthesis of 5-Butyl-4-(4-methoxyphenyl)-6-phenylpyrimidin-2-amine (WQE-134), a Dual Inhibitor of Nitric Oxide and Prostaglandin E2 Production Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-08-28 Pavel Dosoudil; Vladislav Kotek; Viktor Kolman; Ondřej Baszczyňski; Martin Maxmilian Kaiser; Zlatko Janeba; Miroslav Havránek
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High-Throughput Classical Chiral Resolution Screening of Synthetic Intermediates: Effects of Resolving Agents, Crystallization Solvents, and Other Factors Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-08-20 Jun Qiu; Jason M. Stevens
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Development of a Scalable Route for a Highly Polar Heterocyclic Aminocyclopropyl Building Block Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-08-20 Gabriel Schäfer; Muhamed Ahmetovic; Tony Fleischer; Stefan Abele
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Toward a Scalable Synthesis and Process for EMA401, Part I: Late Stage Process Development, Route Scouting, and ICH M7 Assessment Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-08-20 Leo A. Hardegger; Franck Mallet; Barbara Bianchi; Chunlong Cai; Alexandre Grand-Guillaume Perrenoud; Roger Humair; Richard Kaehny; Stephan Lanz; Cheng Li; Jialiang Li; Florian Rampf; Lei Shi; Christoph Spoendlin; Jeannine Stäuble; Shangjun Teng; Xiangguang Tian; Bernhard Wietfeld; Yao Yang; Bo Yu; Christine Zepperitz; Xuesong Zhang; Yong Zhang
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Toward a Scalable Synthesis and Process for EMA401, Part II: Development and Scale-Up of a Pyridine- and Piperidine-Free Knoevenagel–Doebner Condensation Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-08-20 Eric Sidler; Roger Humair; Leo A. Hardegger
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Toward a Scalable Synthesis and Process for EMA401, Part III: Using an Engineered Phenylalanine Ammonia Lyase Enzyme to Synthesize a Non-natural Phenylalanine Derivative Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-08-20 Leo A. Hardegger; Pascal Beney; Dominique Bixel; Christian Fleury; Feng Gao; Alexandre Grand-Guillaume Perrenoud; Xingxian Gu; Julien Haber; Tao Hong; Roger Humair; Andreas Kaegi; Michael Kibiger; Florian Kleinbeck; Van Tong Luu; Lukas Padeste; Florian A. Rampf; Thomas Ruch; Thierry Schlama; Eric Sidler; Anikó Udvarhelyi; Bernhard Wietfeld; Yao Yang
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Improvement of the C-glycosylation Step for the Synthesis of Remdesivir Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-08-05 Fei Xue; Xinbo Zhou; Ruijie Zhou; Xiaohan Zhou; Dian Xiao; Eric Gu; Xiaowen Guo; Ji Xiang; Ke Wang; Likai Yang; Wu Zhong; Yong Qin
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Practical Synthetic Method for Functionalized 1-Methyl-3/5-(trifluoromethyl)-1H-pyrazoles Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-09-02 Maxim A. Tairov; Vitalina Levchenko; Ivan A. Stadniy; Yurii V. Dmytriv; Serhii O. Dehtiarov; Mykola O. Kibalnyi; Anton V. Melnyk; Stanislav Y. Veselovych; Yurii V. Borodulin; Sergey V. Kolotilov; Sergey V. Ryabukhin; Dmitriy M. Volochnyuk
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Synthesis of Dipentaerythritol from Pentaerythritol under Acidic Conditions Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-09-02 Mélissa Landart; Marc Lemaire; Estelle Métay
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Highly Productive α-Alkylation of Ketones with Alcohols Mediated by an Ir–Oxalamidato/Solid Base Catalyst System Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-09-08 Hideo Shimizu; Hironori Maeda; Hideki Nara
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Convenient Continuous Flow Synthesis of N-Methyl Secondary Amines from Alkyl Mesylates and Epoxides Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-08-25 Gary Mathieu; Heena Patel; Hélène Lebel
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Mechanistic Understanding of a Robust and Scalable Synthesis of Per(6-deoxy-6-halo)cyclodextrins, Versatile Intermediates for Cyclodextrin Modification Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-09-10 Susan L. Zultanski; Nadine Kuhl; Wendy Zhong; Ryan D. Cohen; Mikhail Reibarkh; Jon Jurica; Jungchul Kim; Lauren Weisel; Anil R. Ekkati; Artis Klapars; Donald R. Gauthier, Jr.; Jamie M. McCabe Dunn
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Catalytic Oxidation of o-Chlorotoluene with Oxygen to o-Chlorobenzaldehyde in a Microchannel Reactor Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-08-26 Lijun Yang; Peng Liu; Hong-yu Zhang; Yuecheng Zhang; Jiquan Zhao
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A Vilsmeier Chloroformylation by Continuous Flow Chemistry Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-08-17 Manuel Carrera; Laurens De Coen; Michelle Coppens; Wim Dermaut; Christian V. Stevens
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Mini-Monoplant Technology for Pharmaceutical Manufacturing Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-08-26 Brendon J. Doyle; Petteri Elsner; Bernhard Gutmann; Olivier Hannaerts; Christof Aellig; Arturo Macchi; Dominique M. Roberge
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Some Items of Interest to Process R&D Chemists and Engineers Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-08-12 Wenyi Zhao; Sylvain Guizzetti; James A. Schwindeman; David S. B. Daniels; James J. Douglas; Sylvain Petit; Christopher B. Kelly; Alex Kosanovich; John Knight
Email addresses: [email protected]; [email protected]; [email protected]; [email protected]; [email protected]; [email protected]; [email protected]; [email protected]; [email protected]. This article has not yet been cited by other publications.
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Drug Development through Modification of Small Molecular Drugs with Monodisperse Poly(ethylene glycol)s Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-07-22 Tingjuan Wu; Kexin Chen; Shuangyan He; Xiaohe Liu; Xing Zheng; Zhong-Xing Jiang
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Development of a Large-Scale Route to Glecaprevir: Synthesis of the Macrocycle via Intramolecular Etherification Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-07-13 Jeffrey M. Kallemeyn; Kenneth M. Engstrom; Matthew J. Pelc; Kirill A. Lukin; Westin H. Morrill; Haojuan Wei; Timothy B. Towne; Jeremy Henle; Nandkishor K. Nere; Dennie S. Welch; Shashank Shekhar; Matthew M. Ravn; Gang Zhao; Michael G. Fickes; Chen Ding; John C. Vinci; James Marren; Russell D. Cink
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Development of a Large-Scale Route to Glecaprevir: Synthesis of the Side Chain and Final Assembly Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-07-13 David R. Hill; Michael J. Abrahamson; Kirill A. Lukin; Timothy B. Towne; Kenneth M. Engstrom; Rajarathnam E. Reddy; Angelica B. Kielbus; Matthew J. Pelc; Jianzhang Mei; Nandkishor K. Nere; Shuang Chen; Rodger Henry; Sanjay Chemburkar; Chen Ding; Hongqiang Zhang; Russell D. Cink
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Synthesis Development of the Selective Estrogen Receptor Degrader (SERD) LSZ102 from a Suzuki Coupling to a C–H Activation Strategy Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-07-01 Markus Baenziger; Marcel Baierl; Krishnaswamy Devanathan; Sumesh Eswaran; Peng Fu; Bjoern Gschwend; Michael Haller; Gopu Kasinathan; Nikola Kovacic; Audrey Langlois; Yongfeng Li; Friedrich Schuerch; Xiaodong Shen; Yinbo Wan; Regina Wickendick; Siwei Xie; Kai Zhang
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Application of the New 400 MHz High-Temperature Superconducting (HTS) Power-Driven Magnet NMR Technology for Online Reaction Monitoring: Proof of Concept with a Ring-Closing Metathesis (RCM) Reaction Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-07-10 Maria Victoria Silva Elipe; Alan Cherney; Robert Krull; Neil Donovan; Jason Tedrow; Donald Pooke; Kimberly L. Colson
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Biocompatible Catalysts for Lactide Polymerization—Catalyst Activity, Racemization Effect, and Optimization of the Polymerization Based On Design of Experiments Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-07-13 Agnieszka Gadomska-Gajadhur; Paweł Ruśkowski
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A Structured Approach To Cope with Impurities during Industrial Crystallization Development Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-07-06 Stephanie J. Urwin; Guillaume Levilain; Ivan Marziano; Jeremy M. Merritt; Ian Houson; Joop H. Ter Horst
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Improved Scale-up Synthesis and Purification of Clinical Asthma Candidate MIDD0301 Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-07-29 Daniel E. Knutson; M. S. Rashid Roni; Md Yeunus Mian; James M. Cook; Douglas C. Stafford; Leggy A. Arnold
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Practical and Efficient Approach to the Preparation of Diquafosol Tetrasodium Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-06-30 Pengfei Xu; Hai Wang; Pei Shen; Peng Peng; Yongrui Tu; Yongqiang Sun; Jubo Wang; Chenxi Xu; Zhixia Qiu; Raoling Ge; Zhiyu Li; Jinlei Bian
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Novel Si(II)+ and Ge(II)+ Compounds as Efficient Catalysts in Organosilicon Chemistry: Siloxane Coupling Reaction† Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-08-10 Elke Fritz-Langhals; Sven Werge; Sotirios Kneissl; Phillip Piroutek
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Applications of Quantum Chemistry in Pharmaceutical Process Development: Current State and Opportunities Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-07-23 Yu-hong Lam; Yuriy Abramov; Ravi S. Ananthula; Jennifer M. Elward; Lori R. Hilden; Sten O. Nilsson Lill; Per-Ola Norrby; Antonio Ramirez; Edward C. Sherer; Jason Mustakis; Gerald J. Tanoury
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Practical and Efficient Synthesis of 2-Thio-imidazole Derivative—ZY12201: A Potent TGR5 Agonist Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-07-30 Vivek M. Joshi; Chandrakant Sojitra; Santosh Sasane; Mrigendra Shukla; Rakesh Chauhan; Vipin Chaubey; Sarika Jain; Kalpesh Shah; Hemant Mande; Shubhangi Soman; Padmaja Sudhakar Pamidimukkala; Shailesh R. Shah; Bipin Pandey; Kumar K. Singh; Sameer Agarwal
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Performance Analysis and Model-Free Design of Deracemization via Temperature Cycles Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-07-20 Francesca Breveglieri; Iaroslav Baglai; Michel Leeman; Willem L. Noorduin; Richard M. Kellogg; Marco Mazzotti
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Kinetic Investigations To Enable Development of a Robust Radical Benzylic Bromination for Commercial Manufacturing of AMG 423 Dihydrochloride Hydrate Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-07-15 James I. Murray; Maria V. Silva Elipe; Andrew Cosbie; Kyle Baucom; Kyle Quasdorf; Seb Caille
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Controlling a Cohort: Use of Mirabilis-Based Purge Calculations to Understand Nitrosamine-Related Risk and Control Strategy Options Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-06-30 Michael J. Burns; Andrew Teasdale; Eric Elliott; Chris G. Barber
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A General Kilogram Scale Protocol for Suzuki–Miyaura Cross-Coupling in Water with TPGS-750-M Surfactant Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-07-15 Michael Parmentier; Mona Wagner; Regina Wickendick; Markus Baenziger; Audrey Langlois; Fabrice Gallou
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Simple Synthesis of Amides via Their Acid Chlorides in Aqueous TPGS-750-M Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-08-03 Min Shi; Ning Ye; Wei Chen; Hui Wang; Chiming Cheung; Michael Parmentier; Fabrice Gallou; Bin Wu
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Development of a Commercial Manufacturing Route to 2-Fluoroadenine, The Key Unnatural Nucleobase of Islatravir Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-07-31 Cynthia M. Hong; Yingju Xu; John Y. L. Chung; Danielle M. Schultz; Mark Weisel; Richard J. Varsolona; Yong-Li Zhong; Akasha K. Purohit; Cyndi Q. He; Donald R. Gauthier, Jr.; Guy R. Humphrey; Kevin M. Maloney; François Lévesque; Zhixun Wang; Aaron M. Whittaker; Eric Sirota; Jonathan P. McMullen
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Continuous-Flow Synthesis of Cationic Lipid SST-01 via Safe and Scalable Aerobic Oxidation and Reductive Amination Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-07-22 Katsuaki Fujiwara; Haruro Ishitani; Shu̅ Kobayashi
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Electrochemical Cyclobutane Synthesis in Flow: Scale-Up of a Promising Melt-Castable Energetic Intermediate Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-07-27 Longrui Chen; Lisa M. Barton; Julien C. Vantourout; Yinghua Xu; Chengpu Chu; Eric C. Johnson; Jesse J. Sabatini; Phil S. Baran
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Reaction Calorimetry in Continuous Flow Mode: A New Approach for the Thermal Characterization of High Energetic and Fast Reactions Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-07-07 Frederik Mortzfeld; Jutta Polenk; Bertrand Guelat; Francesco Venturoni; Berthold Schenkel; Paolo Filipponi
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A Virtual Plant for Integrated Continuous Manufacturing of a Carfilzomib Drug Substance Intermediate, Part 3: Manganese-Catalyzed Asymmetric Epoxidation, Crystallization, and Filtration Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-07-14 Andrew J. Maloney; Elçin Içten; Gerard Capellades; Matthew G. Beaver; Xiaoxiang Zhu; Lauren R. Graham; Derek B. Brown; Daniel J. Griffin; Rahul Sangodkar; Ayman Allian; Seth Huggins; Roger Hart; Pablo Rolandi; Shawn D. Walker; Richard D. Braatz
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A Virtual Plant for Integrated Continuous Manufacturing of a Carfilzomib Drug Substance Intermediate, Part 2: Enone Synthesis via a Barbier-Type Grignard Process Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-07-14 Elçin Içten; Andrew J. Maloney; Matthew G. Beaver; Xiaoxiang Zhu; Dongying E. Shen; Jo Anna Robinson; Andrew T. Parsons; Ayman Allian; Seth Huggins; Roger Hart; Pablo Rolandi; Shawn D. Walker; Richard D. Braatz
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A Virtual Plant for Integrated Continuous Manufacturing of a Carfilzomib Drug Substance Intermediate, Part 1: CDI-Promoted Amide Bond Formation Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-07-14 Elçin Içten; Andrew J. Maloney; Matthew G. Beaver; Dongying Erin Shen; Xiaoxiang Zhu; Lauren R. Graham; Jo Anna Robinson; Seth Huggins; Ayman Allian; Roger Hart; Shawn D. Walker; Pablo Rolandi; Richard D. Braatz
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