Journal
ORGANIC PROCESS RESEARCH & DEVELOPMENT
Volume 22, Issue 12, Pages 1817-1822Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.oprd.8b00332
Keywords
asymmetric reductive amination (ARA); dynamic kinetic resolution (DKR); iridium; chiral amine
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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.
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