Rh-Catalyzed Borylative Cyclization of Acrylate-Containing 1,6-Enynes

Org Lett. 2023 Aug 4;25(30):5671-5675. doi: 10.1021/acs.orglett.3c02154. Epub 2023 Jul 24.

Abstract

A Rh-catalyzed regioselective, stereoselective carbocyclization/borylation of acrylate-containing 1,6-enynes was described, which offers a general and practical method for constructing versatile and densely functionalized pyrrolidines with the (Z) geometry or the uncommon (E) geometry at the double bond with different substituents of the alkyne, with sterically hindered and conjugative aryl groups favoring the latter, featuring a tetrasubstituted vinyl boronate, containing an all-carbon quaternary stereocenter.