Development and Large-Scale Preparation of an Oral TACE Inhibitor

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• 作者：Scott A. Savage ; Robert E. Waltermire ; Silvio Campagna ; Shailendra Bordawekar ; Joan Dalla Riva Toma
• 刊名：Organic Process Research & Development
• 出版年：2009
• 出版时间：May 15, 2009
• 年：2009
• 卷：13
• 期：3
• 页码：510-518
• 全文大小：190K
• 年卷期：v.13,no.3(May 15, 2009)
• ISSN：1520-586X

文摘

An efficient, expedient synthesis of BMS-561392, 1, which enabled rapid delivery of drug substance for clinical development is described. The key features of the synthesis include an efficient synthesis of a phenolic α,α-disubstituted amino ester via carbon alkylation without protection of the phenol, an effective enzymatic resolution of this racemic amino ester, and a process for the preparation of a hydroxamic acid drug substance with undetectable levels of hydroxylamine.