Ronald J. Post

Chemoselective Saponification in the Synthesis of Danuglipron Facilitated with Trifluoroethanol

Lu Han, Bryan Li, Ke Wang, David B. Damon et autres

Danuglipron (PF-06882961), a potent, orally bioavailable small-molecule glucagon-like peptide-1 receptor (GLP-1R) agonist, is currently being developed for glycemic control among patients with Type-2 diabetes ( J. Med. Chem. 2022, 65, 8208–8226; JAMA Netw. Open. 2023; 6(5): e2314493 ). The earlier synthesis of …

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Kinetic and Data-Driven Reaction Analysis for Pharmaceutical Process Development

Ke Wang, Lu Han, Jason G. Mustakis, Bryan Li et autres

Mathematical modeling of chemical reaction kinetics has been proven to aid the development of new reactions and processes. Chemical kinetic modeling is a well-established principle in chemical engineering that uses fundamental knowledge of the reaction mechanism to predict conversion data. In pharmaceutical …

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The Evolution of High-Throughput Experimentation in Pharmaceutical Development and Perspectives on the Future

Steven M. Mennen, Carolina Alhambra, C. Liana Allen, Mario Barberis et autres

Abstract High-throughput experimentation (HTE) has revolutionized the pharmaceutical industry, most notably allowing for rapid screening of compound libraries against therapeutic targets. The past decade has also witnessed the extension of HTE principles toward the realm of small-molecule process chemistry. Today, most major …

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Palbociclib Commercial Manufacturing Process Development. Part III. Deprotection Followed by Crystallization for API Particle Property Control

Brian P. Chekal, Jason Ewers, Steven M. Guinness, Nathan D. Ide et autres

A three-step commercial manufacturing route has been developed for palbociclib, a highly selective, reversible inhibitor of CDK 4/6. The third step of the palbociclib process is composed of an acid-catalyzed deprotection reaction telescoped through extractive workup and distillation operations into a controlled …

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Development of an Efficient Pd-Catalyzed Coupling Process for Axitinib

Brian P. Chekal, Steven M. Guinness, Brett M. Lillie, Robert W. McLaughlin et autres

The manufacturing process of axitinib ( 1 ) involves two Pd-catalyzed coupling reactions, a Migita coupling and a Heck reaction. Optimization of both of these pivotal bond-formation steps is discussed as well as the approach to control impurities in axitinib. Essential to …

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Public diplomacy in the 21st century: a view from the front lines

Ronald J. Post

ChemInform Abstract: A Direct Synthesis of 3‐(Pyrrolidin‐3‐yl)indoles for Use as Conformationally Restricted Analogues of Tryptamines.

John E. Macor, David H.A. Blank, Kevin B. Ryan, Ronald J. Post

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article …

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ChemInform Abstract: Synthesis and Reactivity of Pyrrolo(3,2‐e)indole: Removal of a N‐BOM Group from an Unactivated Indole.

John E. Macor, James T. Forman, Ronald J. Post, K. M. RYAN

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article …

A Direct Synthesis of 3-(Pyrrolidin-3-yl)indoles for Use As Conformationally Restricted Analogs of Tryptamines

John E. Macor, David H.A. Blank, Kevin B. Ryan, Ronald J. Post

All articles of this category An efficient, two step synthesis of 3-(pyrrolidin-3-yl)indoles 4 is described. Indoles react with maleimides in refluxing acetic acid affording 3-(indol-3-yl)succinimides 6 . Reaction times and yields depend on the substituents on the indole 5 . Direct reduction …

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Synthesis and reactivity of pyrrolo[3,2-e]indole: Removal of a N-BOM group from an unactivated indole

John E. Macor, James T. Forman, Ronald J. Post, Kevin B. Ryan

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ChemInform Abstract: The Discovery of a Novel and Potent Benzodiazepine Receptor Pharmacophore.

John E. Macor, James F. Blake, Kishor Desai, Ronald J. Post et autres

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article …

ChemInform Abstract: 5‐Cyano‐1‐(3‐(N‐methylpyrrolidin‐2R‐ylmethyl)indol‐5‐yl)benzimidazole ( CP‐161,242): A Potent, Centrally Active 5‐HT1D Receptor Agonist and Benzodiazepine Partial Agonist.

John E. Macor, David H.A. Blank, Kishor Desai, Carol B. Fox et autres

Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article …