| 摘要 |
A method for preparing lercanidipine hydrochloride is provided to synthesize the lercanidipine hydrochloride under safe and mild conditions with improved yield through a simplified reaction process. A method comprises the steps of: (a) reacting 2,6-dimethyl-5-methoxycarbonyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3-carboxylic acid represented by the formula(2) with a dialkylchlorophosphate derivative compound represented by the formula(4) to obtain a dialkyl phosphonoester compound represented by the formula(5); and (b) reacting the compound of the formula(5) with 2,N-dimethyl-N-(3,3-diphenylpropyl)-1-amino-2-propanol represented by the formula(3) to obtain lercanidipine hydrochloride represented by the formula(1). In the formulae, R' is O or S, and each R1 and R2 is methoxy, ethoxy, or phenoxy. The obtained lercanidipine hydrochloride is further purified by tetrahydrofuran.
|
