Chiral Magnesium Bisphosphate-Catalyzed Asymmetric Double C(sp³)–H Bond Functionalization Based on Sequential Hydride Shift/Cyclization Process

Abstract

Described herein is a chiral magnesium bisphosphate-catalyzed asymmetric double C(sp3)–H bond functionalization triggered by a sequential hydride shift/cyclization process. This reaction consists of stereoselective domino C(sp3)–H bond functionalization: (1) a highly enantio- and diastereoselective C(sp3)–H bond functionalization by chiral magnesium bisphosphate (first [1,5]-hydride shift), and (2) a highly diastereoselective C(sp3)–H bond functionalization by an achiral catalyst (Yb(OTf)3, second [1,5]-hydride shift).