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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 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
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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
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Thermal Hazard Analysis and Decomposition Mechanism of Energetic Nitration of 4-Methoxy-2-nitroacetanilide Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-03-20 Jiawei Cui, Zhengqi Wu, Ningzhou Shen, Juncheng Jiang
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Rare Case of Polymorphism in the Binary System of Enantiomers of a Praziquantel Derivative Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-03-20 Clément Pinètre, Loïc Ritou, Charline J. J. Gerard, Hugo Cercel, Michel Leeman, Richard M. Kellogg, Paul Tinnemans, Morgane Sanselme, Clément Brandel, Valérie Dupray, Joop H. ter Horst
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A Chiral Pool Strategy for the Synthesis of a SMARCA2 Degrading PROTAC Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-03-20 Miseon Lee, Jiang-Ping Wu, Jaehee Lee, Jun Wang, Jada A. H. White, Kyle W. Rugg, Alexander Sienkiewicz, Jon C. Lorenz, Peter Greb, Matthew H. Bunner, David A. Hirsh, Nina C. Gonnella, Fredrik L. Nordstrom, Christiane Kofink, Harald Weinstabl, Jonathan T. Reeves
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High Enantioselective and Large-Scale Production of Ursodeoxycholic Acid by Combination of Pd- and Hydroxysteroid Dehydrogenase-Catalyzed Hydrogenation Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-03-19 Chunling Zeng, Xirong Liu, Chao Sun, Xinhua Xu, Lifen Peng
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1,2,3-Triazole Synthesis: Development of Safe and Effective Batch and Continuous Manufacturing Processes Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-03-12 Lei Song, Hwee Ting Ang, Jagadeesan Senthilperumal, Umamaheswara Rao Kanusu, Sivasankaran Venugopal, Naveen Rangarajan, Shivasankar Krishnamoorthy, Srinivas Reddy Dubbaka, Patrick O’Neill, Jie Wu
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An Intramolecular Diels–Alder Approach to the Isoindolinone Core of AZD8154 Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-03-13 James J. Douglas, David Buttar, Katharine Locke, Andrew Turner
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Chemistry in Water Reproducibility Study: Learnings from a Precompetitive, Multicompany Collaboration Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-03-15 Richard J. Fox, J. Daniel Bailey, Jennifer Victoriano Obligacion, Niginia Borlinghaus, Wilfried M. Braje, Xiaoyong Li, Subha Mukherjee, Adeline Schoen, Timothy B. Towne, Stella Vukelić
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Thermal Runaway Inhibition of Adipic Acid Green Synthesis Based on a Radical Chain Reaction Mechanism Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-03-15 Jimi Su, Lei Ni, Zhen Cheng, Nan Chen, Peiqing Hao, Dongyan Yang, Yong Pan
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Continuous Flow Chemistry with Solids: A Review Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-03-14 Hannah L. D. Hayes, Carl J. Mallia
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2,5-Dihydro-1H-pyrrol-3-yl Boronic Derivatives: Multigram Synthesis and Coupling Reactions Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-03-13 Oleksandr S. Liashuk, Oleksandr P. Demchuk, Oleksandr V. Hryshchuk, Oleksandr O. Grygorenko
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High-Speed Circulation Flow Platform Facilitating Practical Large-Scale Heterogeneous Photocatalysis Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-03-13 Chenguang Liu, Lei Song, Qiong Liu, Weihao Chen, Jinhui Xu, Mu Wang, Yanbin Zhang, Ting Wei Tan, Zhexuan Lei, Lei Cheng, Saif A. Khan, Jie Wu
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Highly Productive Flow Synthesis for Lithiation, Borylation, and/or Suzuki Coupling Reaction Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-03-13 Hiroki Soutome, Kei Maekawa, Yosuke Ashikari, Aiichiro Nagaki
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Recent Highlights in Micellar Catalysis: An Industrial Outlook Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-03-14 Tharique N. Ansari, Guolin Xu, Andrew Preston, Peng Gao
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Integrated Filtration and Washing Modeling: Optimization of Impurity Rejection for Filtration and Washing of Active Pharmaceutical Ingredients Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-03-12 Bhavik A. Mehta, Ekaterina Gramadnikova, Cameron J. Brown, Niall A. Mitchell, Sara Ottoboni
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Process Development and Kinetic Analysis in the Green Synthesis of Lomustine Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-03-11 Giulia Murbach-Oliveira, Ilke Akturk, Zoltan Nagy, David H. Thompson
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Application of Immobilized Enzymes in Flow Biocatalysis for Efficient Synthesis Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-03-08 Zhongyao Tang, Yuri Oku, Tomoko Matsuda
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Transition-Metal-Free Synthesis of a Densely Functionalized Benzodioxole Intermediate toward Lotiglipron Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-03-12 Jimmy Wang, James Clarke, Matthew Badland, Brian Broadbelt, Louise F. Dow, Harriet A. M. Fenton, Daniel A. Laity, Jinu S. Mathew, Emily K. Rose, Neringa Tamosiunaite, Steven J. R. Twiddle, Robert Walton
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Application of Twin Screw Extrusion to Scale Polymorphs, a Salt, and the Amorphous Phase for Various Drug Substances Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-03-12 Henry Morrison, Peter Fung, Elizabeth Horstman, Olga Lapina, Thoeun Khuth, Diane S. Lye, Christopher S. Regens, Dustin Bringley, Jennifer Alleva
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Rapid Multikilogram Scale-Up of Di- and Trifluoromethoxy Proline Derivatives Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-03-11 Pablo J. Cabrera, Christophe Allais, Joel T. Arcari, María González-Esguevillas, Emma L. McInturff, Matthew R. Reese
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Development of a Directed Ketal Hydrogenation for the Synthesis of a Key Intermediate of Lanabecestat Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-03-09 Rachel H. Munday
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Photochemistry in Pharmaceutical Development: A Survey of Strategies and Approaches to Industry-wide Implementation Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-03-08 Eric G. Moschetta, Gemma C. Cook, Lee J. Edwards, Michael A. Ischay, Zhen Lei, Frederic Buono, François Lévesque, Jeffrey A. O. Garber, Maura MacTaggart, Melda Sezen-Edmonds, Kevin P. Cole, Matthew G. Beaver, Jaika Doerfler, Suzanne M. Opalka, Wenli Liang, Peter D. Morse, Naomi Miyake
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Manufacturing Process Development of Tegoprazan as a Potassium-Competitive Acid Blocker (P-CAB) Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-03-08 Jae-Hong Kweon, Hyungjin Shin, Min Kyoung Lee, Sung Ah Lee, Pargat Singh, Kyeongwon Moon, In Su Kim
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Development of a Scalable Synthesis of a Drug-Linker for ABBV-3373 Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-03-05 Nathan B. Bennett, Bradley D. Gates, Justin A. Simanis, James W. Treadway, Steven M. Richter, Dennie S. Welch
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Some Items of Interest to Process R&D Chemists and Engineers Org. Process Res. Dev. (IF 3.4) Pub Date : 2024-03-05 Alan Steven, Carlos Mateos, Andrei A. Zlota, Alexandre Barthelme, Paul F. Richardson, Robert B. Kargbo, Thomas Verheyen, John Knight
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