Abstract

AbstractAsymmetric detrifluoroacetylative Mannich reactions between α‐fluorinated arylsulfonyl gem‐diols and fluoroalkyl imines have been developed under operationally convenient conditions. Varieties of α‐fluorinated arylsulfonyl gem‐diols and fluoroalkyl imines are well tolerated with the corresponding α‐difluorinated β‐amino sulfone products generated in moderate to excellent yields as well as high diastereoselectivity. The reaction can be reproduced on gram‐scale with uncompromised yield and stereochemical outcome. The synthetic value of the products is demonstrated by two transformations by means of desulfonylation and removal of the sulfinyl protecting‐group.

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