A Simple Access to O-Acyl Bicine

摘要

Bicine,i.e.N,N-bis-(2-hydroxyethyl)glycine is an useful intermediate which may be applied in prodrug strategies,especially for those that can release amine containing bioactive molecules,due to facilitated cyclization of bicine amide 1 to a morpholine lactone 2 at physiological pH with the releasing of ammonia molecule 3.Formation of a morpholine lactone is the driving force in this reaction.