Ir-Catalyzed Regio- and Enantioselective C–H Addition to 1,1-Disubstituted Alkenes Enabled by the Directing Group: Construction of Acyclic Quaternary Stereocenters

Abstract

High Resolution Image Download MS PowerPoint Slide All-carbon quaternary stereocenters are prevalent in many natural products and pharmaceuticals, yet their efficient and selective construction still remains challenging. Here we report iridium-catalyzed regio- and enantioselective hydroheteroarylation of 1,1-disubstituted alkenes. Taking advantage of an appropriate directing group, the all-carbon quaternary stereocenters were constructed with high enantioselectivities. The directing group was easily removed under mild reaction conditions, and thus, the synthetic utility of the product was also demonstrated.

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