METHOD FOR PREPARING GLIBENCLAMIDE

摘要

PURPOSE: Provided is a method for economically synthesizing glibenclamide, with powder shape, which is used as an intermediate for synthesis of medicine useful for treatment of diabetes. CONSTITUTION: The method comprises the steps of (i) reacting N-phenethyl-5-chloro-2-methoxybenzamide with chlorosulfonic acid(ClSO3H) represented by formula 2 in the presence of thionyl chloride(SOCl2) to form p-(N-phenethyl-5-chloro-2-methoxybenzamide)sulfonylchloride represented by formula 3; (ii) reacting sulfonylchloride compound represented by formula 3 with ammonia to form p-(N-phenethyl-5-chloro-2-methoxybenzamide)sulfoneamide represented by formula 4; (iii) reacting sulfoneamide compound represented by formula with alkali metal hydroxide in the presence of alcohol solvent to form p-(N-phenethyl-5-chloro-2-methoxybenzamide)sulfone amide-metal salt represented by formula 5; and (iv) reacting the metal represented by formula 5 with cyclohexyl isocyanate or phenylcyclohexyl carbamate to form glibenclamide represented by formula 1.