Manufacturing Process Development for Belzutifan, Part 5: A Streamlined Fluorination–Dynamic Kinetic Resolution Process

Tao Wang,Eric M. Phillips,Stephen M. Dalby,Eric Sirota,Stephanus Axnanda,C. Scott Shultz, Pratiq Patel,Jacob H. Waldman,Embarek Alwedi,Xiao Wang,Kerstin Zawatzky, Matthew Chow, Nilusha Padivitage,Mark Weisel,Michael Whittington,Jianjun Duan, Taotao Lu

Organic Process Research & Development（2022）

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摘要

Here we report the fluorination–dynamic kinetic resolution (DKR) process for the commercial supply of belzutifan (MK-6482). Key process safety and robustness issues in the Selectfluor fluorination reaction were identified and addressed on the basis of increased mechanistic understanding. Aggressive process optimization enabled a single-pot direct isolation process that allowed delivery of the fluorodiol product with low process mass intensity.

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关键词

fluorination,dynamic kinetic resolution,DKR,Noyori asymmetric reduction,single-pot direct isolation,through-process

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