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

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.