Stereoselective Synthesis of Fused Aziridines via One-Pot Sequential Decarboxylative Mannich Reaction and Oxidative C-H Amination of Cyclic Imines with ß-Ketoacids.

A novel one-pot sequential transformation via decarboxylative Mannich reaction (DMR) and oxidative C-H amination of cyclic imines with ß-ketoacids is described. This methodology has been utilized to provide access to fused aziridines with excellent diastereoselectivity. Several examples of catalytic enantioselective sequential transformation are presented.