It is used to prepare the antidiabetic novel synthesis technique across -4 methylcyclohexylamine base portions of Glimepiride and the derivative salt across the useful intermediate of -4 methylcyclohexylamine hydrochlorides or pivalate

摘要

In the present invention, disclose a kind of preparation method, for general formula V across -4 methylcyclohexylamine, optionally show the general formula VII of the transisomer of high-content general formula VIII or pivalate one accordingly across -4 methylcyclohexylamine hydrochlorides, wherein preparation process is characterized in that following steps: a) making the Schiff base of general formula to isomerization, by handling it in the case where the isomery that the highly basic in the solvent selected from aliphatic ether, cyclic ethers, dialkylsulfoxides or dialkyl sulfone class obtains general formula X; B) make the isomery of general formula to acidolysis, by handling it in the case where an inorganic acid obtains the corresponding salt across -4 methylcyclohexylamine; C) optionally a base portion of the salt of the acquisition across -4 methylcyclohexylamine to general formula V or the hydrochloride of VIII pivalate of general formula of general formula VII. The compound of general formulae V, VII or VIII are used to prepare Glimepiride.