Studies On Asymmetric Mannich Reaction Ofα-Phenylsulfonylmethylene Phosphonates Catalyzed By Organocatalysts

In this thesis, a series of small molecule organocatalysts have been designed and synthesized for the asymmetric Mannich reaction of N-Boc aromatic aldimine with a-phenylsulfonylmethylene phosphonates. After preliminary catalyst screening and optimizating reaction conditions, it was found that the bulky quaternary ammonium phase transfer catalyst15derived from cinchona alkaloid could achieve some extent of enantioselectivity (up to67%ee) and good diastereoselectivity (up to84:16dr), while only give a low yield. In order to get a better result, the reaction conditions are still being further optimized.