Studying On Asymmetric Mannich Reaction Of α-Diazomethylphosphonates To Ketimines Derived From Isatins

In this thesis, a series of bifunctional chiral (thio)ureas, squaramides and BINOL-derived phosphonic acids with substituents on C3and C3’of BINOL have been synthesized and used for the asymmetric Mannich-type reaction of imines derived from Isatins and a-diazomethylphosphonates. After screening the catalysts and optimizing the reaction conditions, such as base, temperature, solvent, catalyst loading, it was found that the ligand L30combined with Ag2CO3was capable of promoting the reaction with good yields (76%) and enantioselectivities (up to90%) when the reaction performed in toluene at-30℃with5mol%L30and Ag2CO3(1:1).