Synthesis of 4-phosphono-beta-lactams via phosphite addition to acyliminium salts

摘要

4-Aryl-4-phosphono-beta-lactams are prepared by acylation of iminium salts with chloroacetyl chloride followed by phosphite addition and ring closure using sodium hydride as a base. Deacylation of the iminium salt is in competition with the desired addition of phosphites to acyliminium salts, which lowers the yield of the reaction.