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

The non-enzymatic kinetic resolution of diversely substituted primary propargylic amines is reported featuring a highly selective acetyl transfer using (1S,2S)- 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).