Concise synthesis of α-amino cyclic boronates via multicomponent coupling of salicylaldehydes, amines, and B2(OH)4

Abstract

We report here a concise synthesis of α-amino cyclic boronates via multicomponent coupling of readily available salicylaldehydes, amines, and B₂(OH)₄. The process can be carried out at room temperature in ethanol, does not require catalysts or additives, and is easy to scale up. Aminals and ligated boroxines are intermediates in this reaction.