期刊
ORGANIC PROCESS RESEARCH & DEVELOPMENT
卷 25, 期 4, 页码 960-968出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.oprd.1c00004
关键词
vadadustat; process; development; scalable
资金
- State Key Laboratory of Anti-Infective Drug Development (Sunshine Lake Pharma Co., Ltd) [2015DQ780357]
A novel and scalable process has been developed for the industrial synthesis of vadadustat, achieving a total yield of 49.1% with a purity of >99.5%. The process, optimized through various steps, has been demonstrated at kilogram scale and the impurity profile has been extensively studied and documented.
A novel and scalable process is developed for the industrial synthesis of vadadustat. The four-step process is one step shorter compared to the reported routes with an increase in total yield to 49.1%. Detailed optimizations furnish vadadustat with a purity of >99.5% through cross-coupling, aromatic substitution and nitrile hydrolysis, amidation, and ester-ether deprotection. The process is also robust and was demonstrated in a kilogram laboratory. Meanwhile, the corresponding impurity profile was thus studied in detail and well documented.
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