Kinetic resolution of propargylamines via a highly enantioselective non-enzymatic N-acylation process

Abstract

The non-enzymatic kinetic resolution of diversely substituted primary propargylic amines is reported featuring a highly selective acetyl transfer using (1S,2S)-1 in conjunction with Aliquat^TM 336, affording the corresponding enantio-enriched N-acetylated propargylic amines with unprecedented levels of selectivity (s-factors of up to 193 at 50% conversion).