Iodine-Mediated δ-Amination of sp3 C-H Bonds

J Org Chem. 2024 Mar 1;89(5):3481-3490. doi: 10.1021/acs.joc.3c02901. Epub 2024 Feb 21.

Abstract

We present a direct δ-amination reaction of sp3 C-H bonds, employing molecular iodine (I2) as the sole oxidant under transition-metal-free conditions. This remote C-H functionalization approach is operationally simple and provides facile, efficient access to pyrrolidines and related heterocyclic derivatives from readily accessible substrates.