American Chemical Society
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Sulfur-Directed α‑C(sp3)–H Amidation of Pyrrolidines with Dioxazolones under Rhodium Catalysis

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journal contribution
posted on 2023-12-22, 19:39 authored by Pargat Singh, Jeonghyun Min, Sujin Min, Kyeongwon Moon, Hyung Sik Kim, In Su Kim
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.