| Michael reaction as one of the most powerful and efficient methods for the formation of carbon-carbon bonds in organic synthesis has attracted great attention in the past decades. Recently, with the scope of this field rapidly expanding, Many enantioselective Michael reactions that form optical active carbon-carbon, carbon-oxygen, carbon-sulfur and carbon-nitrogen bond have been reported, which expand the applications of Michael Reaction in the field of total synthesis.Dihydropyridines(DHPs) are analogues of NADH coenzymes and important class of bioactive molecules in the field of drug and pharmaceuticals. The synthesis of DHPs have been reported by some research groups. however, only one group reported the synthesis of optical active DHPs by now. we have developed a highly enantioselective organocatalytic asymmetric Michael reaction ofβ-enaminocarbonyl derivatives andα,β-unsaturated aldehydes to prepare 4-substituded DHPs With optical activity in the presence of a secondary amine catalyst, which is easily prepared from proline. The method should be very useful in the synthesis of optical active DHPs. |
