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Pilot-Scale Operation and Characterization of an Organolithium-Mediated Coupling Reaction in Flow to Form a Ketone Intermediate on the Route to Nemtabrutinib Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-05-09 Robert D. Franklin, Travis Armiger, Douglas A. L. Otte, Reed T. Larson, Glenn Spencer, Pratiq A. Patel, Mellie June Paulines, Jackson R. Hall, Kai-Jiong Xiao, Patrick S. Fier, Vailankanni L. Rodrigues, Erik D. Guetschow, Nadine Kuhl, Lisa Jellett, James Corry, Cheol K. Chung, David A. Thaisrivongs
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Development of a Green and Sustainable Manufacturing Process for a Key Intermediate to Nemtabrutinib (MK-1026): Sequential Deprotonation–Lithiation as a Batch–Flow Process Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-05-09 Douglas A. L. Otte, Reed T. Larson, Embarek Alwedi, Travis Armiger, Yonggang Chen, Cheol K. Chung, James Corry, Richard Desmond, Patrick S. Fier, Robert D. Franklin, Erik D. Guetschow, Jackson R. Hall, Holst M. Halsey, Clara Hartmanshenn, Lisa Jellett, Nadine Kuhl, François Lévesque, Jonathan P. McMullen, Pratiq A. Patel, Mellie June Paulines, Hong Ren, Vailankanni L. Rodrigues, Serge Ruccolo, Lushi
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Development of Lab-Scale Continuous Stirred-Tank Reactor as Flow Process Tool for Oxidation Reactions Using Molecular Oxygen Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-05-08 Ursina Gnädinger, Dario Poier, Claudio Trombini, Michal Dabros, Roger Marti
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Development of a Scalable Alkylation via a Protection/Deprotection Sequence for BMT-773752: Key Intermediate in the Synthetic Route to Repotrectinib Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-05-08 Han Zhang, Binfeng Li, Jin Yang, Changchun Xu, Rafaela Carmona, Jason Zhu, Bilal Hoblos, Steven Wisniewski
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Continuous Crystallization Kinetics of Cefradine in a Mixed Suspension Mixed Product Removal System Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-05-07 Yueyi Yang, Chenxin Xie, Chuang Ma, Baoshu Liu, Xiaowei Cheng, Hongxun Hao, Hua Sun
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Design and Characterization of a Novel Continuous Annular Gap Crystallizer Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-05-07 Nico Nys, Lorenz Buchgraber, Peter Neugebauer, Matthew J. Jones, Heidrun Gruber-Woelfler
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Scalable Protocol for Removing Triphenylphosphine Oxide from Reactions Using MgCl2 and Wet Milling Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-05-07 Eric G. Moschetta, Benoit Cardinal-David, Travis B. Dunn, Moiz Diwan
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Efficient, Scalable Synthesis of Functionalized Pyrrolo[2,1-f][1,2,4]triazines Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-05-07 Shawn K. Pack, Lei Feng, Ce Chen, Zhongzhen Li
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A Coalescing Filter for Liquid–Liquid Separation and Multistage Extraction in Continuous-Flow Chemistry Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-05-06 James Daglish, A. John Blacker, Gregory de Boer, Stephen J. Russell, Muhammad Tausif, David R. J. Hose, Anna R. Parsons, Alex Crampton, Nikil Kapur
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Kilogram-Scale Synthesis of 11β-Hydroxyandrosterone Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-05-06 Hossay Abas, Peter Blencowe, Ellen MacDonald, Emma Stanway, Eric P. A. Talbot, Haiyang Wang, Morag Watson, Jin Zhang, Lucy A. Harwood
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Continuous Scalable Synthesis and Concentration Variation of Organozinc Compounds Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-05-02 Lars Gössl, Kai Dahms, Gabriele Menges-Flanagan, Michael Maskos
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Development of a Kilogram-Scale Manufacturing Route for Bis-Tac-dG: Essential Building-Block for Guadecitabine Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-05-03 Kirtee Wani, Shyamapada Banerjee, Nipun Davar, Yogesh S. Sanghvi
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Enantioselective Synthesis in Continuous Flow: Polymer-Supported Isothiourea-Catalyzed Enantioselective Michael Addition–Cyclization with α-Azol-2-ylacetophenones Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-05-02 Zhanyu Zhou, Kevin Kasten, Tengfei Kang, David B. Cordes, Andrew D. Smith
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Some Items of Interest to Process R&D Chemists and Engineers Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-05-02 Alan Steven, Carlos Mateos, Andrei A. Zlota, Alexandre Barthelme, Paul F. Richardson, Robert B. Kargbo, Thomas Verheyen, Christopher C. Nawrat, Sylvain Guizzetti, John Knight
This article has not yet been cited by other publications.
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Comprehensive Review on the Synthetic Strategies toward Anti-SARS-CoV-2 Drug Ensitrelvir Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-05-01 Yuanchang Liu, Gaorong Wu, Yiting Yang, Wei Hu, Xiaopeng Peng, Zihan Peng, Jiatao Xia, Xin Xie, Jiuzhong Huang, Weiming Chen
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Impurity Profiling for a Scalable Continuous Synthesis and Crystallization of Carbamazepine Drug Substance Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-05-01 Matthew Glace, Harrison Kraus, Wei Wu, David Acevedo, Dongxia Liu, Thomas D. Roper, Adil Mohammad
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Analytical Strategy for Low-Level Estimation of Unstable Genotoxic Boronate Ester Impurities Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-04-30 Bhoopendra Singh Kushwah, Santosh Gandhi, Devikumar Purandharan, Ashok Kumar Rajendran, Karthik Jayaraman, Venkata Phanikrishna Sharma Mangalampalli, Joel Young, Lakshmikant Bajpai
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Mechanistic Studies of Imidazole Autocatalysis in 1,1′-Thiocarbonyldiimidazole-Mediated Couplings of Aniline Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-04-30 Nathan March, Bradley J. Paul-Gorsline
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Development of a Mechanism-Based Kinetic Model and Process Optimization Incorporating Imidazole Autocatalysis in a 1,1′-Thiocarbonyldiimidazole-Mediated Thiocarbonyl Transfer Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-04-30 Bradley J. Paul-Gorsline
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Semicontinuous Temperature Cycle-Induced Deracemization Using an Axially Chiral Naphthamide Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-04-30 Ryusei Oketani, Riku Naito, Ichiro Hisaki
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Impact of ICH Q11 Questions and Answers on the Outcome of Active Pharmaceutical Ingredient Starting Material Proposal Acceptance by ICH Regulatory Members Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-04-29 Steven Tymonko, Brenda J. Burke, Jean-Philippe Crochard, Olivier Dirat, Kenneth J. Fraunhoffer, Cristian Harrison, Timothy Kramer, Heewon Lee, Vlad Liberman, Kanwar P. S. Sidhu, Randi Smith, Neil A. Strotman, Nil Tandogan, Alan Triman, Haitao Zhang
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Selective Thermal Deprotection of N-Boc Protected Amines in Continuous Flow Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-04-25 Michelle-Rose Ryan, Denis Lynch, Stuart G. Collins, Anita R. Maguire
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Efficient Synthesis of (S)-Nornicotine using Co-Immobilized IRED and GDH in Batch and Continuous Flow Reaction Systems Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-04-25 Senling Guan, Wenfeng Zhou, Yongtang Yue, Songhe Wang, Bo Chen, Haishen Yang
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An Easy and Adjustable One-Pot Access to Pheromonal Blends of Fall Armyworm (Spodoptera frugiperda) Relying on a Key Ligand- and Additive-Free Iron-Catalyzed Cross-Coupling Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-04-23 Pablo Chourreu, Olivier Guerret, Eric Gayon, Guillaume Lefèvre
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Development of the Synthetic Route to PF-06878031 Part 2: Amide Reduction Route Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-04-19 Maria S. Brown, Julia Buck, Douglas J. Critcher, Andrew M. Derrick, Harriet Fenton, Steven J. Fussell, Adam E. S. Gymer, Michael Hawksworth, Heather Ingram, Rebecca A. Johnson, Rajesh Kumar, Daniel A. Laity, Russell D. Lewis, Jinu S. Mathew, Laura McGivern, Ian B. Moses, Andrew T. Palaia, Miheal J. Patel, James Rellegue, Emily K. Rose, Adam Scott, Jeremy Steflik, Steven J. R. Twiddle
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Development of the Synthetic Route to PF-06878031 Part 1: Selective Alkylation Route Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-04-19 Oriana Brea, Julia Buck, Nessa Carson, Andrew M. Derrick, Steven J. Fussell, Adam E. S. Gymer, Michael Hawksworth, Adam W. Hopkins, Heather Ingram, Rebecca A. Johnson, Daniel A. Laity, Jinu S. Mathew, Ian B. Moses, James Rellegue, Emily K. Rose, Steven J. R. Twiddle, Adam West
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Commercial Route Development Toward PF-07265807, an AXL-MER Inhibitor Oncology Candidate Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-04-16 Douglas J. Critcher, Christopher Paul Ashcroft, Alan J. Pettman, Matthew Badland, Robert Szpera, William Waddington
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What Does It Take to Develop Structurally Complex Molecules by Total Synthesis? Rapid Process Development and GMP Manufacturing of E7130 Drug Substance for First-in-Human Clinical Study Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-04-15 Takeo Sasaki, Kenzo Yahata, Minetaka Isomura, Isao Ohashi, Takashi Fukuyama, Yusuke Miyashita, Yuzo Watanabe, Norio Murai, Masaaki Matsuda, Atsushi Kamada, Yosuke Kaburagi, Kazunobu Kira, Kentaro Iso, Yuki Sato, Fumiyoshi Matsuura, Yasunobu Matsumoto, Hiroshi Azuma, Daisuke Iida, Tasuku Ishida, Wataru Itano, Satoshi Nagao, Masashi Seki, Akihiko Yamamoto, Yuji Yamamoto, Naoki Yoneda, Masayuki Matsukura
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Oligonucleotide Purification by Ion Exchange Chromatography: A Step-by-Step Guide to Process Understanding, Modeling, and Simulation Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-04-11 Kilian Kobl, Lucrèce Nicoud, Edouard Nicoud, Anna Watson, John Andrews, Edward A. Wilkinson, Muhid Shahid, Christopher McKay, Benjamin I. Andrews, Batool Ahmed Omer, Olga Narducci, Edward Masson, Suzanne H. Davies, Tobias Vandermeersch
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Integrated Continuous-Flow Production of Wax Esters Combining Whole-Cell and In Vitro Biocatalysis Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-04-11 Supacha Buttranon, Juthamas Jaroensuk, Pimchai Chaiyen, Nopphon Weeranoppanant
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Adagrasib’s Second-Generation Synthesis: Transitioning from Route Scouting to Optimization Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-04-10 Zhichao Lu, Chengsheng Chen, Dinesh J. Paymode, Yonghong Gan, Thomas Scattolin, Sahar Roshandel, Weitong Dong, Stanley Yu, Stéphane Lemeune, David R. Snead, Cheng-yi Chen
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A Facile Method for Multigram Scale Light-Induced Synthesis of 4′-(Bromomethyl)-2-cyanobiphenyl Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-04-10 Steffen G. Sveegaard
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Overriding Innate Decomposition Temperatures of an Avibactam Prodrug Precursor Using Data Science-Guided Synthesis Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-04-10 Jacob Werth, Michael Butler, Jenson Verghese, Nga M. Do, Lacey Samp, Remzi Duzguner, Michele T. Buetti-Weekly
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Development of a Continuous Process for the Large-Scale Asymmetric Manufacture of (R)-3-Methoxy-2-(4-methylpiperazin-1-yl)propanoic Acid Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-04-08 Carl J. Mallia, Peter R. Moore, Simon Hardy, Christopher D. Parsons, Paul A. J. Cronin, Andrew Ikin, Carl-Johan Aurell, Kuangchu Dai, Baoquan Sun
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Total Synthesis with Gram-Scale Radical Process: An Inspiration for Pharmaceutical Industry Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-04-09 Shaomin Fu, Bo Liu
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Facile Generation of tert-Butoxycarbonyl Chloride Equivalent and Its Use in Microflow Reactor Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-04-08 Kana Miyamoto, Ren Okabe, Shinichiro Fuse
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Some Items of Interest to Process R&D Chemists and Engineers Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-04-08 James A. Schwindeman, Alex Kosanovich, Christopher B. Kelly, Timothy Kwok, Thomas James, Annabel Q. Ansel, James M. MacDougall, Jimmy Lauberteaux, John Knight
This article has not yet been cited by other publications.
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Catalysis and Synthesis Enabled by P-Chiral Dihydrobenzooxaphosphole Ligands Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-04-08 Zhen Cao, Dongyang He, Wenjun Tang
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Kinetic Study and Model-Based Design Space Determination for a Drug Substance Flow Synthesis Using an Amination Reaction via Nucleophilic Aromatic Substitution Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-04-04 Junu Kim, Yusuke Hayashi, Sara Badr, Kazuya Okamoto, Toshikazu Hakogi, Haruo Furukawa, Satoshi Yoshikawa, Hayao Nakanishi, Hirokazu Sugiyama
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Practical Manufacturing Process for Baloxavir Marboxil: Efficient Route to a Tricyclic Triazinanone Scaffold Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-04-03 Nobuaki Fukui, Toshikatsu Maki, Kazunori Ban, Akihito Kijima, Setsuya Shibahara, Kazuya Okamoto, Sho Kamiya, Tatsuro Yasukata, Takayuki Tsuritani
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Practical Manufacturing Process for Baloxavir Marboxil: Effective Selection and Replacement of Protective Group toward Enhancement of Crystallization-Induced Diastereomer Transformation Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-04-04 Nobuaki Fukui, Setsuya Shibahara, Toshikatsu Maki, Tatsuhiko Ueno, Shuichi Yanagisawa, Kazuya Okamoto, Emi Tanimoto, Takafumi Ohara, Tatsuro Yasukata, Takayuki Tsuritani
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First-Generation Process Development for the Synthesis of Baloxavir Marboxil: Early-Stage Development of Synthetic Methods to Prepare Baloxavir Marboxil Intermediates Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-04-03 Kosuke Anan, Masayoshi Miyagawa, Azusa Okano, Hideki Sugimoto, Naoki Miyake, Nobuaki Fukui, Akihito Kijima, Emi Tanimoto, Makoto Kawai
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ANFIS-Driven Machine Learning Automated Platform for Cooling Crystallization Process Development Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-04-04 Cha Yong Jong, Akshay Mittal, Geordi Tristan, Vanessa Noller, Hui Ling Chan, Yongkai Goh, Eunice Wan Qi Yeap, Srinivas Reddy Dubbaka, Harsha Rao Nagesh, Shin Yee Wong
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Streamlining Catalysis Screenings on a Budget Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-04-02 Pascal Czember, Florian Weber, Agon Kokollari, Hubert Spreitzer, Nico Fleck
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Striving for Uniformity: A Review on Advances and Challenges To Achieve Uniform Polyethylene Glycol Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-04-01 Cláudia Bento, Marianna Katz, Maria M. M. Santos, Carlos A. M. Afonso
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Practical Synthesis of 6-Amino-1-hydroxy-2,1-benzoxaborolane: A Key Intermediate of DNDI-6148 Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-03-29 Pankaj V. Khairnar, John M. Saathoff, Daniel W. Cook, Samuel R. Hochstetler, Urvish Pandya, Stephen J. Robinson, Vijay Satam, Kai O. Donsbach, B. Frank Gupton, Li-Mei Jin, Charles S. Shanahan
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Development of a Safe and Scalable Method to Prepare 3-Bromo-N-alkyl-1,6-naphthyridones via Enamine Cyclization Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-03-29 Thomas Carr, Sam Beddoe, Stephen Johns, Jonathan Hull, Tom Stowe, Jonathan Moore, James Brown, Adrian Maddaford, Etienne Rochette, Michel Bernatchez, Martin Jean, Jean Francois Parent, Connor Barrett, Jeffrey B. Sperry, Daniel Richter
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Synthesis and Crystallization Research of Voclosporin Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-03-29 Bibo Jiang, Jiajia Liu, Ying Li, Zidan Mai, Liya Lin, Shengjun Xu, Yongfu He, Fei Chen, Jianfen Shao, Chuanmeng Zhao, Fuli Zhang
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Efficient Multikilogram-Scale Synthesis of PTDSS1 Inhibitor: Development of a Practical and Scalable Optical Resolution Method for Chiral 2,3-Pyrrolidinedione Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-03-26 Keisuke Suzuki, Ryusei Itoh, Jo Oyama, Masaki Hayashi, Tsuyoshi Ueda
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A Tandem Ring Closure and Nitrobenzene Reduction with Sulfide Provides an Improved Route to an Important Intermediate for the Anti-Tuberculosis Drug Candidate Sutezolid Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-03-27 Hanuman P. Kalmode, Ongolu Ravikumar, Dinesh J. Paymode, John Bachert, Justina M. Burns, Rodger W. Stringham, Sarah L. Aleshire, Ryan C. Nelson
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Development and Scale-Up of a Key Copper-Catalyzed Biaryl Ether Formation for the Multikilogram Synthesis of Emprumapimod Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-03-26 Christopher Brearley, Robert David Bright, James Clarke, Douglas J. Critcher, Susana Torres, Ingrid Edwards, Harriet Fenton, Shanjun Huang, Rebecca Amy Johnson, Ricky A. Jones, Suju P. Mathew, Rhys Norster, Kathryn Alice Starbuck, Amelia Taylor-Young, William Waddington, Robert Walton, Jimmy Wang
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QbD Approach to Process Characterization and Quantitative Criticality Assessment of Process Parameters† Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-03-25 Pankaj D. Rege, Andreas Schuster, Jens Lamerz, Christian Moessner, Wolfgang Göhring, Pirmin Hidber, Helmut Stahr, Oana Mihaela Andrei, Janine Burren, Alexandre Moesching, Daniel Coleman, Stefan Hildbrand
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A New Process To Prepare Thiophene-2-Carbonyl Chloride, a Key Raw Material in the Synthesis of Tioxazafen, Utilizing a Catalytic Liquid Phase Aerobic Oxidation Reaction Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-03-25 Daniel P. Walker, Kevin J. Koeller, William H. Miller, Charles R. Graham, G. Davis Harris, Jr., Swati Nigudkar, George H. Klemm, Wensheng Li
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A Short Review on the Synthetic Routes for the Antiepileptic Drug (S)-Levetiracetam Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-03-23 Sayantan Paul, Asish K. Bhattacharya
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Biocatalyst Immobilization and Process Intensification: Production of (S)-Piperazine-2-carboxylic Acid Dihydrochloride Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-03-19 David Roura Padrosa, Dennis Wetzl, Stefan Hildbrand, Paolo Tosatti, Joerg Sedelmeier, Kurt Puentener, Hans Iding, Francesca Paradisi
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Identification, Synthesis, Characterization, and Control Strategy Establishment for Process Impurities of Baloxavir Marboxil Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-03-22 Huixiong Lu, Guobin Xu, Jingping Kou, Shuming Wu, Jiebin Zeng, Yuting Liu, Jidi Lin, Yongbo Xu, Wei Shang, Yaoyao Li, Zhongqing Wang
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Mechanistic Evidence for Mild Base-Mediated Intermolecular Trans-Aminoacylations of 1-Acyl-5-amino-1H-1,2,4-triazoles and 5-Amino-1H-1,2,4-triazoles to Afford 5-Acylamino-1H-1,2,4-triazoles Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-03-22 Nicholas A. Magnus, Natalie G. Franklin-Charlesworth, Jesús González, James C. Muir
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Organic Solvent Nanofiltration in Pharmaceutical Applications Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-03-22 Hui Xiao, Yanyue Feng, William R. F. Goundry, Staffan Karlsson
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Recent Advances in Nonprecious Metal Catalysis Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-03-21 Andrew R. Ickes, Michael C. Haibach, Nicholas G. W. Cowper, Tonia S. Ahmed
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Research and Development on the Manufacturing Process of Dexmedetomidine from Chiral Precursors: Resolution–Racemization–Recycle Synthesis Strategy Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-03-20 Dmitry Orekhov