Traceless Thioacid-Mediated Radical Cyclization of 1,6-Dienes

J Org Chem. 2023 Jul 21;88(14):10020-10026. doi: 10.1021/acs.joc.3c00824. Epub 2023 Jul 7.

Abstract

Five-membered ring systems are ubiquitous throughout natural products and synthetic therapeutics, and thus, efficient methods to access this essential scaffold are required. Herein, we report the thioacid-mediated, 5-exo-trig cyclization of various 1,6-dienes, with high yields of up to 98%. The labile thioester functionality can be exploited to generate a free thiol residue which can be used as a functional handle or removed entirely to provide the traceless cyclized product.