Copper-Catalyzed Intermolecular Carbosulfonylation of Alkynes to Access Functionalized Eight-Membered Tetrahydroazocines.

Authors

Ran Ding, Jia-Nan Zhao, Pan-Ya Cui, Pei-Li Li, Zi-Rong Li, Hui Gao

Published in

The Journal of organic chemistry. Jul 05, 2026. Epub Jul 05, 2026.

Abstract

A copper-catalyzed tandem sulfonylation-cyclization of 3-aza-1,7-enynes with sulfonyl chlorides was developed for the efficient synthesis of sulfonylated eight-membered tetrahydroazocines in good yields and with excellent functional group compatibility. The regio- and chemoselective addition of sulfonyl radicals onto the alkynes of the tertiary enamide moiety triggers a cascade reaction followed by 8-endo cyclization, resulting in the generation of tetrahydroazocine derivatives. This transformation demonstrated a novel and efficient pathway to form eight-membered azocines, accompanied by the incorporation of a useful sulfone group.

PMID:
42402142
Bibliographic data and abstract were imported from PubMed on 05 Jul 2026.

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