Manufacturing Process Development for Belzutifan, Part 1: A Concise Synthesis of the Indanone Starting Material

Feng Peng,Lushi Tan, Lu Chen,Stephen M. Dalby,Daniel A. DiRocco,Jianjun Duan, Minyi Feng, Guan Gong, Haiheng Guo,J. Caleb Hethcox, Lu Jin,Heather C. Johnson,Jungchul Kim, Diane Le,Yipeng Lin,Wenjun Liu, Jun Shen, Yimei Wan,Chengqian Xiao,Bangping Xiang, Qun Xiang, Jing Xu, Luliang Yan, Weiyi Yang,Honglin Ye, Yanpei Yu, Jun Zhang

Organic Process Research & Development（2022）

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摘要

A four-step synthesis of the indanone core of belzutifan (MK-6482) is described. This route starts from the commodity raw material dihydrocoumarin and was successfully demonstrated on a large scale to produce indanone 11 in the synthesis of belzutifan, an FDA-approved first-in-class therapy for the treatment of patients with certain types of Von Hippel–Lindau disease-associated tumors.

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关键词

belzutifan,Friedel−Crafts cyclization,CuBr-promoted sulfonylation

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