Abstract:

With lipase Novozym435 as catalyst, ethyl acetate as solvent as well as acyl donor, the crucial intermediatesS(+)3-methyl-1-(2-(1-piperidinyl)phenyl) butylamine of Repaglinide was synthesized enzymatically with a total yield of 17%. Compared with chemical catalysts, the enzymatic resolution method has higher enantioselectivity, regioselectivity and substrate specificity. The synthetic route is easy to operate under a moderate condition with less secondary reaction. Enzyme can be reutilized after activation, which reduces cost, and thus applied to industrial production.

Key words:  synthesis promoted by enzyme, Repaglinide intermediate, lipase Novozym435, pharmaceutical chemistry