Oxidative Coupling of Primary Benzamide with Alkenes via o-CH Activation Mediated by Cu(II)/Ru(II)

J Org Chem. 2024 Dec 6;89(23):17752-17760. doi: 10.1021/acs.joc.4c00637. Epub 2024 Nov 13.

Abstract

A selective ortho-olefination of primary amides yields valuable motifs for pharmaceuticals. Primary amide-directed ortho-olefination of benzamide using unactivated alkenes was successfully conducted with a ruthenium(II) catalyst. The established protocol demonstrates efficacy across various benzamides, achieving moderate to good yields with high functional group tolerance. Furthermore, the transformation of ortho-olefinated amides into five-membered lactams highlights their synthetic applicability in the pharmaceutical sector.