Access to gem-Difluoro Olefins via C-H Functionalization and Dual Role of Anilines

Org Lett. 2020 Sep 18;22(18):7234-7238. doi: 10.1021/acs.orglett.0c02568. Epub 2020 Aug 31.

Abstract

In this Letter, we describe a simple, practical approach in which cheap CuI was used as a catalyst to introduce a gem-difluoro olefin onto simple electron-rich aniline derivatives in good yield via direct C-H functionalization and a subsequent HF elimination reaction. Detailed mechanistic studies point at a dual role of aniline derivatives in this reaction, which serve as a substrate and a basic promoter to trigger the HF elimination step.