Oxidative Tandem Cyclization of Glycine Esters with Propargyl Alcohols

J Org Chem. 2023 Jul 21;88(14):10232-10241. doi: 10.1021/acs.joc.3c00627. Epub 2023 Jul 9.

Abstract

A facile and efficient aerobic oxidative (4 + 2)-cyclization/aromatization/lactonization tandem reaction of N-aryl glycine esters with propargyl alcohols to access quinoline-fused lactones is reported. The reaction can be extended to homopropargylic alcohols too. The transformation is straightforward to perform under mild conditions and scalable, and both reaction components are readily available.