Copper-Catalyzed Intramolecular C-H Alkoxylation of Diaryltriazoles: Synthesis of Tricyclic Triazole Benzoxazines

Org Lett. 2020 Jul 17;22(14):5320-5325. doi: 10.1021/acs.orglett.0c01517. Epub 2020 Jun 26.

Abstract

An efficient copper-catalyzed intramolecular C-H alkoxylation of 1,4-disubstituted 1,2,3-triazoles has been developed. The chemistry was applied to a wide range of substrates, generating tricyclic benzoxazine-fused 1,2,3-triazoles in good yields. Mechanistic studies suggest that a radical pathway may be involved in this transformation. The triazole products were found to exhibit strong antifungal activity against ginseng root-rot disease, demonstrating their potential as a scaffold in medicinal chemistry research.

Publication types

  • Research Support, Non-U.S. Gov't