Sulfur-Directed α-C(sp3)-H Amidation of Pyrrolidines with Dioxazolones under Rhodium Catalysis

Org Lett. 2024 Jan 12;26(1):57-61. doi: 10.1021/acs.orglett.3c03633. Epub 2023 Dec 22.

Abstract

Site-selective functionalization of saturated N-heterocycles such as pyrrolidines is a central topic in organic synthesis and drug discovery. We herein report the sulfur-assisted rhodium(III)-catalyzed sp3 C-H amidation of pyrrolidines with dioxazolones as amidating agents. The amenability of the thioamide directing group is elucidated by a series of control experiments.