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

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

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 t...

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Veröffentlicht in:Organic letters 2024-01, Vol.26 (1), p.57-61
Hauptverfasser: Singh, Pargat, Min, Jeonghyun, Min, Sujin, Moon, Kyeongwon, Kim, Hyung Sik, Kim, In Su
Format: Artikel
Sprache:eng
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Zusammenfassung: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.
ISSN:1523-7060
1523-7052
DOI:10.1021/acs.orglett.3c03633