摘要 |
A process for preparing lercanidipine hydrochloride is provided, thereby improving yield by performing the process under mild condition in the presence of a coupling reagent, simplifying the process, and easily removing a by-product using water, so that the lercanidipine hydrochloride can be simply and stably mass produced. The process for preparing lercanidipine hydrochloride represented by formula (1) comprises reacting 2,6-dimethyl-5- methoxycarbonyl-4- (3-nitrophenyl)- 1,4-dihydropyridine- 3-carboxylic acid of formula (2) with 2,N-dimethyl-N- (3,3-diphenylpropyl)- 1-amino-2-propanol of formula (3) in the presence of 2-chloro-1,3-dimethylimidazolium chloride of formula (4) as a coupling reagent and base in solvent at 10 to 60 deg. C, wherein the solvent is selected from dichloromethane, 1,2-dichloroethane and chloroform; and the base is pyridine, trimethylamine and triethylamine.
|