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Development of a Novel Chemoenzymatic Process for (S)-1-(Pyridin-4-yl)-1,3-propanediol Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-11-25 Hong-Yi Wang; Jia-Wei Tang; Peng Peng; Hai-Jun Yan; Fu-Li Zhang; Shao-Xin Chen
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Accelerated Development of a Scalable Ring-Closing Metathesis to Manufacture AMG 176 Using a Combined High-Throughput Experimentation and Computational Modeling Approach Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-11-25 Gabrielle St-Pierre; Alan H. Cherney; Wencan Chen; Xiaofei Dong; Peter K. Dornan; Daniel J. Griffin; K. N. Houk; Janice B. Lin; Stephen Osgood; Maria V. Silva Elipe; Heath C. Timmons; Yong Xie; Jason S. Tedrow; Oliver R. Thiel; Austin G. Smith
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Synthesis of Vixotrigine, a Voltage- and Use-Dependent Sodium Channel Blocker. Part 2: Development of a Late-Stage Process Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-11-25 Robbie Chen; Vincent Couming; John Guzowski, Jr.; Erwin Irdam; William F. Kiesman; Daw-Iong Albert Kwok; Wenli Liang; Tamera Mack; Erin M. O’Brien; Suzanne M. Opalka; Daniel Patience; Stefan Sahli; Donald G. Walker; Frederick Osei-Yeboah; Chaozhan Gu; Xin Zhang; Markus Stöckli; Thiemo Stucki; Hanspeter Matzinger; Roman Kuhn; Michael Thut; Markus Grohmann; Benjamin Haefner; Joerg Lotz; Michael Nonnenmacher;
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Efficient Method for the Synthesis of Amino-1,3-Oxazines from Thioureas Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-11-24 Jeffery Richardson; Peter J. Lindsay-Scott; Vladimir Larichev; Emily Pocock
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Design of a Kilogram Scale, Plug Flow Photoreactor Enabled by High Power LEDs Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-11-24 François Lévesque; Michael J. Di Maso; Karthik Narsimhan; Michael K. Wismer; John R. Naber
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Synthesis of Vixotrigine, a Use-Dependent Sodium Channel Blocker. Part 1: Development of Bulk Supply Routes to Enable Proof of Concept Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-11-24 Gerard Giblin; Adrian Heseltine; William Kiesman; David MacPherson; James Ramsden; Ravi Vadali; Michael Williams; David Witty
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Process Research and Scale-Up Synthesis of 3-(4-Isobutyl-2-methylphenyl)propanal, a Safe and Uniquely Performing Perfumery Ingredient Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-11-24 Martin A. Lovchik; Chi-Lam Tse; Simon Ellwood
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Risk-Based Operation of a Continuous Mixed-Suspension-Mixed-Product-Removal Antisolvent Crystallization Process for Polymorphic Control Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-11-23 Iben Ostergaard; Heidi Lopez de Diego; Haiyan Qu; Zoltan K. Nagy
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Precise Preparation of a High-Purity Key Intermediate of Tazobactam Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-11-23 Yanan Zhou; Chengjun Wu; Hongzhi Ma; Jianchao Chen; Tiemin Sun
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Development of a Scalable Synthesis of trans-4-Fluorocyclohexylamine via Directed Hydrogenation Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-11-23 Joyce C. Leung; Thach T. Nguyen; Mariusz Krawiec; Donghong A. Gao; Jonathan T. Reeves
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Some Items of Interest to Process R&D Chemists and Engineers Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-11-11 Kiran Matcha; 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]; [email protected]. This article has not yet been cited by other publications.
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A Primer for Pharmaceutical Process Development Chemists and Analysts in Relation to Impurities Perceived to Be Mutagenic or “Genotoxic” Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-11-05 David J. Snodin
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Recent Advances in Nonprecious Metal Catalysis Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-10-30 Michael C. Haibach; Andrew R. Ickes; Alison M. Wilders; Shashank Shekhar
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Development of a Green and Sustainable Manufacturing Process for Gefapixant Citrate (MK-7264) Part 1: Introduction and Process Overview Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-10-16 Hong Ren; Kevin M. Maloney; Kallol Basu; Michael J. Di Maso; Guy R. Humphrey; Feng Peng; Richard Desmond; Douglas A. L. Otte; Embarek Alwedi; Wenjun Liu; Si-Wei Zhang; Siqing Song; Rebecca A. Arvary; Michael A. Zompa; Dan Lehnherr; Gary E. Martin; Hsieh Yao D. Chang; Anne E. Mohan; Francisco J. Guzman; Lisa Jellett; Alfred Y. Lee; Glenn Spencer; Elizabeth S. Fisher; John R. Naber; Hong Gao; Sachin
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Development of a Green and Sustainable Manufacturing Process for Gefapixant Citrate (MK-7264) Part 2: Development of a Robust Process for Phenol Synthesis Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-10-16 Feng Peng; Guy R. Humphrey; Kevin M. Maloney; Dan Lehnherr; Mark Weisel; Francois Lévesque; John R. Naber; Andrew P. J. Brunskill; Patrick Larpent; Si-Wei Zhang; Alfred Y. Lee; Rebecca A. Arvary; Claire H. Lee; Daniel Bishara; Karthik Narsimhan; Eric Sirota; Michael Whittington
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Development of a Green and Sustainable Manufacturing Process for Gefapixant Citrate (MK-7264) Part 3: Development of a One-Pot Formylation–Cyclization Sequence to the Diaminopyrimidine Core Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-10-20 Kallol Basu; Dan Lehnherr; Gary E. Martin; Richard A. Desmond; Yu-hong Lam; Feng Peng; John Y. L. Chung; Rebecca A. Arvary; Michael A. Zompa; Si-Wei Zhang; Jinchu Liu; Zachary E. X. Dance; Patrick Larpent; Ryan D. Cohen; Francisco J. Guzman; Nicholas J. Rogus; Michael J. Di Maso; Hong Ren; Kevin M. Maloney
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Development of a Green and Sustainable Manufacturing Process for Gefapixant Citrate (MK-7264) Part 4: Formylation–Cyclization as a Flow–Batch Process Leads to Significant Improvements in Process Mass Intensity (PMI) and CO Generated versus the Batch–Batch Process Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-11-05 Douglas A. L. Otte; Kallol Basu; Lisa Jellett; Michael Whittington; Glenn Spencer; Matthew Burris; Emily B. Corcoran; Kevin Stone; Jarod Nappi; Rebecca A. Arvary; David Donoghue; Hong Ren; Kevin M. Maloney; John R. Naber
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Development of a Green and Sustainable Manufacturing Process for Gefapixant Citrate (MK-7264). Part 5: Completion of the API Free Base via a Direct Chlorosulfonylation Process Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-10-20 Michael J. Di Maso; Hong Ren; Si-Wei Zhang; Wenjun Liu; Richard Desmond; Embarek Alwedi; Karthik Narsimhan; Alexei Kalinin; Patrick Larpent; Alfred Y. Lee; Sumei Ren; Kevin M. Maloney
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Development of a Green and Sustainable Manufacturing Process for Gefapixant Citrate (MK-7264). Part 6: Development of an Improved Commercial Salt Formation Process Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-10-23 Kevin M. Maloney; Si-Wei Zhang; Anne E. Mohan; Alfred Y. Lee; Patrick Larpent; Hong Ren; Guy R. Humphrey; Richard Desmond; Michael DiBenedetto; Wenjun Liu; Ivan H. Lee; Eric Sirota; Michael J. Di Maso; Embarek Alwedi; Siqing Song; Hsieh Yao D. Chang
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Understanding API Static Drying with Hot Gas Flow: Design and Test of a Drying Rig Prototype and Drying Modeling Development Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-10-16 Sara Ottoboni; Simon J. Coleman; Christopher Steven; Mariam Siddique; Marine Fraissinet; Marion Joannes; Audrey Laux; Alastair Barton; Paul Firth; Chris J. Price; Paul A. Mulheran
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Chemical Reaction of Carbon Dioxide with Bisepoxides for Synthesis of Organic Cyclic Dicarbonates at Ambient Pressure for Polyhydroxy Urethane Synthesis Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-10-28 Michael Schmitt; Veronika Strehmel
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Process Safety in the Pharmaceutical Industry—Part I: Thermal and Reaction Hazard Evaluation Processes and Techniques Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-10-24 Ayman D. Allian; Nisha P. Shah; Antonio C. Ferretti; Derek B. Brown; Stanley P. Kolis; Jeffrey B. Sperry
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Development of a Scalable Synthesis of Mevidalen (LY3154207), an Orally Available Positive Allosteric Modulator of the Human Dopamine D1 Receptor Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-09-22 Jeffery Richardson; Kevin P. Cole; Amy C. DeBaillie; Junliang Hao; Jared Piper; Peter Houghton; John Rizzo; Mo Jia; Peng Liu; Ping Huang; Katarina Kadlecikova; Conchita F. Garcia; Daniel S. Richards
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An Improved Process for the Manufacture of 5′-O-(4,4′-Dimethoxytrityl)-N2-isobutyryl-2′-O-(2-methoxyethyl)guanosine Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-09-23 Andrew K. McPherson; Daniel Capaldi; Lijian Chen; Philip Olsen
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Quantitative Perspective on Online Flow Reaction Profiling Using a Miniature Mass Spectrometer Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-11-10 Huaming Sheng; Emily B. Corcoran; Zachary E. X. Dance; Joseph P. Smith; Zhihao Lin; Victoria Ordsmith; Simon Hamilton; Ping Zhuang
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Facile Preparation of 4-(4-Nitrophenyl)morpholin-3-one via the Acid-Catalyzed Selective Oxidation of 4-(4-Nitrophenyl)morpholine by Sodium Chlorite as the Sole Oxidant Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-09-14 Chaoyang Liu; Tao Yu; Tiannuo Yang; Haozhou Sun; Cheng Qin; Qiang Jia; Changhu Chu
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Development of Manufacturing Processes for the Carboxylic Acid Key Intermediate of Lusutrombopag: One-Pot Reaction Process of Formylation and the Horner–Wadsworth–Emmons Reaction Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-09-22 Takaharu Matsuura; Yusuke Sato; Yutaka Nishino; Tadafumi Komurasaki; Yoshiaki Imamura; Makoto Kakinuma
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Chemoenzymatic Process for the Preparation of (S)-7-((tert-Butyldiphenylsilyl)oxy)hept-1-yn-4-ol in a Continuous Packed-Bed Reactor, a Key Intermediate for Eribulin Synthesis Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-09-22 Avula Shiva Krishna; Shalini Basetty; Rajesh Nasam; Samuel L. Ralte; Chada Raji Reddy; Gangarajula Sudhakar; Srihari Pabbaraja; Srivari Chandrasekhar; Prathama S. Mainkar; Thenkrishnan Kumaraguru; Subhash Ghosh
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Continuous Industrial-Scale Centrifugal Partition Chromatography with Automatic Solvent System Handling: Concept and Instrumentation Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-11-06 László Lorántfy; Dóra Rutterschmid; Róbert Örkényi; Dávid Bakonyi; József Faragó; Gergő Dargó; Árpád Könczöl
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Process Development of Sotagliflozin, a Dual Inhibitor of Sodium–Glucose Cotransporter-1/2 for the Treatment of Diabetes Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-10-07 Matthew M. Zhao; Haiming Zhang; Shinya Iimura; Mark S. Bednarz; Qiu-Ling Song; Ngiap-Kie Lim; Jie Yan; Wenxue Wu; Kuangchu Dai; Xiaodong Gu; Youchu Wang
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Crystallizing Fats? Development of a Scalable, Chromatography-Free Synthesis of Cationic Lipids Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-10-19 Gregory L. Beutner; Sloan Ayers; Shawn Brueggemeier; Patricia Cho; Ronald Carrasquillo-Flores; Kathleen Kelly; Federico Lora Gonzalez; Jonathan Marshall; Subha Mukherjee; Jun Qiu; Michael J. Smith
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Solubility Behaviors and Correlations of Common Solvent–Antisolvent Systems Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-10-14 Jun Qiu; Jacob Albrecht; Jacob Janey
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Short Gram-Scale Synthesis of Sulfavant A Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-10-16 Marcello Ziaco; Laura Fioretto; Genoveffa Nuzzo; Angelo Fontana; Emiliano Manzo
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Developing a Multistep Continuous Manufacturing Process for (1R,2R)-2-Amino-1-methylcyclopentan-1-ol Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-10-28 Shengquan Duan; Xichun Feng; Miguel Gonzalez; Scott Bader; Cheryl Hayward; Tomislav Ljubicic; Jiangping Lu; Jason Mustakis; Mark Maloney; Joseph Rainville; Xin Zhang
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Ruthenium-Catalyzed Ester Reductions Applied to Pharmaceutical Intermediates Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-11-11 Youssef Shaalan; Lee Boulton; Craig Jamieson
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Recent Advances in High-Throughput Automated Powder Dispensing Platforms for Pharmaceutical Applications Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-10-23 Matthew N. Bahr; Mark A. Morris; Noah P. Tu; Aakankschit Nandkeolyar
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Development of a Quality Risk Based Tool for the Selection of Regulatory Starting Materials for Commercial Drug Substance Manufacturing Processes Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-11-05 John Lepore; Tariq Mahmood; Robert Hartman
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Merging Biocatalysis, Flow, and Surfactant Chemistry: Innovative Synthesis of an FXI (Factor XI) Inhibitor Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-11-09 Bin Wu; Sisi Zhang; Tao Hong; Yizong Zhou; Hui Wang; Min Shi; Hongwei Yang; Xiangguang Tian; Jing Guo; Jianwei Bian; James Roache; Pete Delgado; Ruowei Mo; Cary Fridrich; Feng Gao; Jianhua Wang
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Practical and Scalable Manufacturing Process for Plasma Kallikrein Inhibitor ASP5069 Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-11-16 Shun Hirasawa; Yoshinori Kohmura
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Catalysis-Based Fluorometric Method for Trace Palladium Detection with Improved Convenience Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-11-12 Jessica M. Williams; Annelise K. Wanner; Kazunori Koide
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Development of Scalable Routes to 1-Bicyclo[1.1.1]pentylpyrazoles Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-11-10 Cayetana Zarate; Michael Ardolino; Gregori J. Morriello; Kaitlyn M. Logan; William P. Kaplan; Luis Torres; Derun Li; Meng Chen; Hongming Li; Jing Su; Peter Fuller; Matthew L. Maddess; Zhiguo Jake Song
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Tandem Continuous Flow Curtius Rearrangement and Subsequent Enzyme-Mediated Impurity Tagging Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-11-06 Marcus Baumann; Alexander Leslie; Thomas S. Moody; Megan Smyth; Scott Wharry
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Formulation of Diacerein Cocrystal Using β-Resorcylic Acid for Improvement of Physicomechanical and Biopharmaceutical Properties Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-10-28 Rajeshri D. Patel; Mihir K. Raval
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Scalable, Telescoped Hydrogenolysis–Enzymatic Decarboxylation Process for the Asymmetric Synthesis of (R)-α-Heteroaryl Propionic Acids Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-10-28 Caroline A. Blakemore; Scott P. France; Lacey Samp; Deane M. Nason; Eddie Yang; Roger M. Howard; Karen J. Coffman; Qingyi Yang; Aaron C. Smith; Edelweiss Evrard; Wei Li; Linlin Dai; Lixia Yang; Zhiguang Chen; Qingli Zhang; Fangyan He; Jiesen Zhang
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Design and Commercialization of an End-to-End Continuous Pharmaceutical Production Process: A Pilot Plant Case Study Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-10-21 Christopher J. Testa; Chuntian Hu; Khrystyna Shvedova; Wei Wu; Ridade Sayin; Federica Casati; Bhakti S. Halkude; Paul Hermant; Dongying Erin Shen; Anjana Ramnath; Qinglin Su; Stephen C. Born; Bayan Takizawa; Saptarshi Chattopadhyay; Thomas F. O’Connor; Xiaochuan Yang; Sukumar Ramanujam; Salvatore Mascia
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Flow Chemistry Enabling Efficient Synthesis Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-10-16 John R. Naber; C. Oliver Kappe; Jaan A. Pesti
This article is part of the Flow Chemistry Enabling Efficient Synthesis special issue. Flow chemistry, continuous processing, continuous manufacturing—a field with nearly as many names as applications—has continued to expand over the last 10 years. The idea of continuous input of starting materials connected to continuous removal of product from a process is neither a new concept nor constrained to
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Seeding Techniques and Optimization of Solution Crystallization Processes Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-09-15 Yang He; Zhenguo Gao; Teng Zhang; Jie Sun; Yiming Ma; Ningning Tian; Junbo Gong
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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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Zinc-Catalyzed Alkylation of Aromatic Amines in Continuous Flow Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-09-14 Le Zhang; Xiaofan Bo; Hanlin Yao; Mengmei Mao; Li Wan; Zhong Xin
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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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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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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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Optimization and Scale-Up of the Continuous Flow Acetylation and Nitration of 4-Fluoro-2-methoxyaniline to Prepare a Key Building Block of Osimertinib Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-10-06 Manuel Köckinger; Benjamin Wyler; Christof Aellig; Dominique M. Roberge; Christopher A. Hone; C. Oliver Kappe
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Polymer-Supported Chiral Cis-Disubstituted Pyrrolidine Catalysts and Their Application to Batch and Continuous-Flow Systems Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-10-06 Hidenori Ochiai; Akira Nishiyama; Naoki Haraguchi; Shinichi Itsuno
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Use of High-Throughput Tools for Telescoped Continuous Flow Synthesis of an Alkynylnaphthyridine Anticancer Agent, HSN608 Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-10-06 Shruti A. Biyani; Qingqing Qi; Jingze Wu; Yuta Moriuchi; Elizabeth A. Larocque; Herman O. Sintim; David H. Thompson
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Synthesis of a Crizotinib Intermediate via Highly Efficient Catalytic Hydrogenation in Continuous Flow Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-09-29 Feng Xu; Jianli Chen; Xiaoxuan Xie; Pengfei Cheng; Zhiqun Yu; Weike Su
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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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Continuous Flow C-Glycosylation via Metal–Halogen Exchange: Process Understanding and Improvements toward Efficient Manufacturing of Remdesivir Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-09-24 Timo von Keutz; Jason D. Williams; C. Oliver Kappe
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Some Items of Interest to Process R&D Chemists and Engineers Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-10-06 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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Toward the Scale-Up of a Bicyclic Homopiperazine via Schmidt Rearrangement and Photochemical Oxaziridine Rearrangement in Continuous-Flow Org. Process Res. Dev. (IF 3.023) Pub Date : 2020-10-15 Michael Brown; Mohammed Aljarah; Hannah Asiki; Leo M. H. Leung; Deborah A. Smithen; Natalie Miller; Gabor Nemeth; Lawrence Davies; Dan Niculescu-Duvaz; Alfonso Zambon; Caroline Springer
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