| 摘要 |
A process for preparing lercanidipine hydrochloride is provided to improve the preparation yield through a simple process under safe and mild conditions by performing the preparation through one pot reaction with dialkylchloro phosphate derivatives, and enhance the economical efficiency by using inexpensive materials. A process for preparing lercanidipine hydrochloride represented by the formula(1) comprises the steps of: reacting 2,6-dimethyl-5-methoxycarbonyl-4-(3-nitrophenyl)-1,4-dihydropyridin-3-carboxylic acid represented by the formula(2) with dialkylchlorophosphate derivatives represented by the formula(4) to prepare dialkylphosphonoester compounds represented by the formula(5); and reacting the dialkylphosphonoester compounds represented by the formula(5) with 2,N-dimethyl-N-(3,3-diphenylpropyl)-1-amino-2-propanol represented by the formula(3), wherein R' is oxygen or sulfur atom, and R1 and R2 are the same or different and each independently methoxy, ethoxy or phenoxy group.
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