Asymmetric Hydroesterification of Diarylmethyl Carbinols

Abstract

Abstract An efficient asymmetric hydroesterfication of diarylmethyl carbinols is developed for the first time with a Pd‐WingPhos catalyst, resulting in a series of chiral 4‐aryl‐3,4‐dihydrocoumarins in excellent enantioselectivities and good yields. The method features mild reaction conditions, a broad substrate scope, use of easily accessible starting materials, and low palladium loadings. A plausible stereochemical model is also proposed with the Pd‐WingPhos catalyst. This method has enabled a 4‐step asymmetric synthesis of ( R )‐tolterodine from readily available starting materials.

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