The invention relates to a 2-substituted vinylsulfonate compound, and preparation method and use thereof in the field of chemical industry of drugs. The 2-substituted vinylsulfonate compound has the following structure formula: FORMULA, wherein R1 and R2 are substituted aromatic groups, R3 is alkyl substituted aromatic group, n1 is any one of integers of 1 to 4, n2 is 0, 1 or 2, X is O, substituted alkyl or aromatic group, and Y is any one of O, S, C and NH. The invention also relates to a preparation method of the compound and the use of the compound in preparing drug for inhibiting activity of PTPlB protein. The compound can be used for preparing drug for treating or preventing diabetes or obesity taking PTPlB as target point.