Study on the Asymmetric Organocatalytic Synthesis of Hydroxymethyl Thiapyrone Derivatives
Two organocatalysts with multiple hydrogen bonds and active centers,(S)-2-hydroxy-N-(pyrroline-2-methylene)benzamide(1a)and(S)-3-hydroxy-N-(pyrroline-2-methylene)-2-naphthylamide(1b),were synthesized from proline and used for the syn-thesis of hydroxymethyl thiapyrone derivatives.Research result shows that using dichloromethane as the solvent,room temperature 25 ℃,and 15 mol％1a as the catalyst,the synthesized hydroxythiopyrone derivatives have a good yield(89％)and a high enantioselectivity(92％).This method provides an important pathway for the synthesis of biopharmacologically active hydroxymethyl thiapyrones.
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