Uncatalyzed One‐Pot Diastereoselective Synthesis of α‐Amino Phosphonates Under Solvent‐Free Conditions

Abstract

Abstract Uncatalyzed one‐pot, three‐component reactions of aldehydes, chiral α‐methylamines, and dimethyl phosphite under solvent‐free conditions were used for the diastereoselective synthesis of α‐amino phosphonates. The reactions proceeded with extremely high efficiency under mild conditions and gave good yields and diastereoselectivities (70:30 to 93:7 dr ). This approach could be useful for the large‐scale synthesis of several α‐amino phosphonates.