Rh-Catalyzed Ortho C-H Alkynylation of Aromatic Aldehydes

Org Lett. 2021 Feb 19;23(4):1263-1268. doi: 10.1021/acs.orglett.0c04243. Epub 2021 Feb 9.

Abstract

The Rh(III)-catalyzed ortho-alkynylation of benzaldehydes is enabled by the transient formation of an imine as a directing group. A broad scope of substrates was obtained under mild reaction conditions, granting access to mono- and dialkynylated products. The functionalization of readily available building blocks allowed the development of modular syntheses of dibenzopentalenes, isoquinolines, indoles, and indolines.