期刊
ORGANIC PROCESS RESEARCH & DEVELOPMENT
卷 22, 期 12, 页码 1817-1822出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.oprd.8b00332
关键词
asymmetric reductive amination (ARA); dynamic kinetic resolution (DKR); iridium; chiral amine
We report the first example of a catalytic asymmetric reductive amination under dynamic kinetic resolution (DKR) conditions for the preparation of a chiral amine as a key intermediate toward Tofacitinib, an active pharmaceutical ingredient developed by Pfizer. Such a protocol allows the preferential formation of a single product out of four possible diastereomers of the chiral amine starting from the corresponding racemic ketone. The chiral iridium catalyst able to perform such a feast was discovered through a mix of high-throughput screening, racemization study, and reaction optimization.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据