Metal-free remote site-selective radical C(sp3)–H acyloxylation of amides

Abstract

The acyloxylation is a highly versatile transformation in synthetic chemistry. While numerous transition metal-catalyzed methods have been developed for C(sp3)–H activation to form C–OCOR bonds, direct acyloxylation of unactivated C(sp3)-H bonds under metal-free conditions remains underexplored. Here, we report a method for the direct acyloxylation of unactivated C(sp3)–H bonds employing photo-induced and the 1,5-HAT process. This approach features broad substrate scope, excellent functional group compatibility, and complete regioselectivity