α-Amino-C-phosphinic acids and derivatives are an important group of compounds of synthetic and medicinal interest and particular attention has been dedicated to their stereoselective synthesis in recent years. Among these, phosphinic pseudopeptides have acquired pharmacological importance in influencing physiologic and pathologic processes, primarily acting as inhibitors for proteolytic enzymes where molecular stereochemistry has proven to be critical. This review summarizes the latest developments in the asymmetric synthesis of acyclic and phosphacyclic α-amino-C-phosphinic acids and derivatives, following in the first case an order according to the strategy used, whereas for cyclic compounds the nitrogen embedding in the heterocyclic core is considered. In addition selected examples of pharmacological implications of title compounds are also disclosed.The authors gratefully acknowledge the CONACYT (grant 181816, 248868) and PRODEP
(project UAEMOR-PTC-379) of Mexico, Ministerio de Economía y Competitividad (grant CTQ2013-40855-R) and
Gobierno de Aragón-FSE (research group E40) for their financial support.We acknowledge support by the CSIC Open Access Publication Initiative through its Unit of Information Resources for Research (URICI)
