Early Development and Kilogram Scale-Up of a Non-steroidal FXR Agonist for the Treatment of Non-alcoholic Steatohepatitis (NASH)

Greg T. Cizio, Kathy Dao, Edward M. Doerffler, Nolan D. Griggs,Michael A. Ischay, Baldip S. Kang, Matthew M. Logan, Patricia D. MacLeod, Adam B. Weinstein, Lok Him L. Yu

Organic Process Research & Development（2022）

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摘要

Non-alcoholic steatohepatitis (NASH) is a serious chronic liver disease characterized by progressive fibrosis that can lead to cirrhosis, liver failure, and death. Compound 1 is a farnesoid X receptor (FXR) agonist that was investigated for use as a treatment for NASH. This paper describes process development efforts enabling the first multikilogram scale-up.

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关键词

FXR agonist,magnesium−halogen exchange,alkylation,SNAr,azetidine,hydrolysis

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