Chemical Development of the Casein Kinase I-Epsilon Inhibitor: 3-(3-Fluorophenyl) sulfanyl-1 H-pyrrolo [3, 2-b] pyridine-2-carboxylic Acid Amide

…, G Kubiak, JJ Shay, C Pemberton, J Peers…

Index: Huang, Bao-Guo; Kubiak, Gregory; Shay, John J.; Pemberton, Clive; Peers, James; Hanna, Reda G.; Powers, Matthew R.; Gamboa, Juan A.; Gelormini, Ann M.; Yarabe, Hyacinthe; Rudisill, Duane E. Organic Process Research and Development, 2011 , vol. 15, # 5 p. 1040 - 1045

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Citation Number: 2

Abstract

The development of a scalable process for 3-arylsulfanyl-1 H-pyrrolo [3, 2-b] pyridine-2- carboxylic acid amides (1), potent casein kinase I inhibitors, is described. The rapid identification of suitable reaction conditions expedited the lab scale synthesis of drug substances for early toxicological evaluations. Further improvements were made to achieve a safe and cost-effective process to meet increasing demands for drug substances to ...