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

The development of a scalable process for 3-arylsulfanyl-1H-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 eval...

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Published inOrganic process research & development Vol. 15; no. 5; pp. 1040 - 1045
Main Authors 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
Format Journal Article
LanguageEnglish
Published American Chemical Society 16.09.2011
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Summary:The development of a scalable process for 3-arylsulfanyl-1H-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 support clinical studies. This paper describes the synthesis at multikilogram scale.
ISSN:1083-6160
1520-586X
DOI:10.1021/op200171a