An efficient one-pot synthesis of bis(α-aminoalkyl)phosphinic acids, phosphorus-isosteric analogues of HIV protease inhibitors

An acid-catalyzed three-component reaction between hypophosphorous acid, aldehydes and alkyl carbamates under mild conditions afforded bis(α-aminoalkyl)phosphinic acids. The proposed facile single-stage protocol is prospective for expansion of a range of phosphinic analogues of HIV protease inhibitors.