The Research Of Catalytic Asymmetric Henry Reaction Of 2-acylpyridine N-oxides

The asymmetric construction of chiral quaternary stereocenters is a considerable challenge in modern organic synthesis.The formation of chiral quaternary stereocenters is of great importance for the synthesis of enantiomerically pure natural products and pharmaceuticals.The Henry(nitroaldol)reaction of ketones has become one of the most important and versatile reactions for the construction of β-nitro-tertiary alcohol containing hydroxyl and nitro groups today.The enantioselective addition of nitroalkanes to 2-Acylpyridine N-Oxides allows the preparation of optically pure β-Nitro-tertiary alcohol which has pyridine compounds.Besides,pyridine derivatives have great importance for the medical,agrochemical and chemical industry.More than 7000 drugs featuring this heterocyclic ring are circulating on the world market,such as herbicides,fungicides,or bactericides.We have developed a novel asymmetric Henry reaction of 2-acypyridine N-oxides catalyzed by a Ni-aminophenol sulfonamide complex,obtained varied quaternary carbons compounds containing pyridine.The result showed in 26-99% yield with 18-99% ee.