Pd-Catalyzed Deacylative [4 + 1] Annulation of N-Arylimidoyl Chlorides with β-Keto Esters Leading to 2-Fluoroalkyl Indoles

J Org Chem. 2024 Sep 20;89(18):13795-13799. doi: 10.1021/acs.joc.4c01709. Epub 2024 Sep 10.

Abstract

A palladium-catalyzed [4 + 1] annulation of N-arylimidoyl chlorides with β-keto esters has been developed. In the presence of Pd(OAc)2, PCy3, and K3PO4, a variety of fluoalkyl-containing N-arylimidoyl chlorides smoothly underwent the cascade C-H imidoylation/deacylative Heck-type reactions to afford biologically important 2-fluoroalkyl indoles in moderate to good yields.