Oxaziridine‐Mediated Oxyamination of Indoles: An Approach to 3‐Aminoindoles and Enantiomerically Enriched 3‐Aminopyrroloindolines

Abstract

A radical solution: A highly regioselective copper(II)-catalyzed oxyamination of N-acyl indoles with oxaziridines gave aminal products that could be converted in a single step into 3-aminoindoles and 3-aminopyrroloindolines (see scheme). When a chiral N-acyl group was used, the core fragment of some architecturally fascinating pyrroloindoline alkaloids was formed with 91 % ee. Bs=benzenesulfonyl, Moc=methoxycarbonyl.