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Preparation method of lercanidipine

A technology of lercanidipine and dimethyl, applied in the field of preparation of lercanidipine, can solve the problems of complex manufacturing process and high production cost, and achieve the effects of simple manufacturing process, low cost and high output

Inactive Publication Date: 2015-07-01
李磊
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the current production process of Lercanidipine, the manufacturing process is complicated and the production cost is high

Method used

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Embodiment Construction

[0006] The present invention will now be described in further detail.

[0007] The preparation method of lercanidipine of the present invention, the specific steps are as follows: 2,6-dimethyl-5-methoxycarbonyl-4-(3-nitrophenyl)-1,4-dihydropyridine -3-carboxylic acid is dissolved in anhydrous dichloromethane and anhydrous dimethylformamide, under the protection of nitrogen, thionyl chloride is added dropwise, and the temperature is controlled at -4~+1℃, and the mixture is stirred for 1h after dropping. At -10~0℃, add dropwise anhydrous dichloromethane solution of 2,N-dimethyl-N-(3,3-diphenylpropyl)-1-amino-2--alcohol. After stirring at 0°C for 3h, then place it at room temperature for 18-20h, evaporate the solvent under reduced pressure, and dissolve the residue in ethyl acetate. Use saturated brine, 10% sodium carbonate solution, saturated brine, 1mol / L hydrochloric acid and saturated Wash with brine, dry, filter, add carbon to the filtrate, filter again, concentrate the filtra...

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PUM

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Abstract

The invention relates to a preparation method of lercanidipine. The preparation method comprises the following steps of dissolving 2,6-dimethyl-5-methoxycarbonyl-4-(3-nitrophenyl)-1,4-dihydropyridyl-3-carboxylic acid in waterless dichloromethane and waterless dimethylformamide, dropwisely adding thionyl chloride into the solution under control of a temperature in a range of -4 to 1 DEG C, then carrying out stirring for 1h, dropwisely adding an anhydrous methylene chloride solution of 2,N-dimethyl-N-(3,3-dibenzylpropyl)-1-amino-2-ol into the mixed solution at a temperature of -10 to 0 DEG C, then carrying out stirring at a temperature of 0 DEG C for 3h, standing the mixture at a room temperature for 18-20h, carrying out washing orderly by saturated salt water, a sodium carbonate solution with a concentration of 10%, saturated salt water, hydrochloric acid with content of 1mol / L and saturated salt water, adding lercanidipine hydrochloride seed crystals into the washed product, carrying out standing at a temperature of 0-5 DEG C for 1d, carrying out filtration and carrying out anhydrous ethanol re-crystallization to obtain lercanidipine hydrochloride. The preparation method of lercanidipine has the advantages of simple preparation processes, high yield and low cost.

Description

Technical field [0001] The present invention relates to the field of pharmaceutical preparation, in particular to a preparation method of lercanidipine. Background technique [0002] Lercanidipine is a third-generation dihydropyridine calcium channel blocker. Its mechanism of action is similar to that of similar drugs. It can reversibly block the Ca2+ influx of L-type calcium channels in vascular smooth muscle cell membranes, dilate peripheral blood vessels and lower blood pressure. Due to the current production process of lercanidipine, the manufacturing process is complex and the production cost is high. Contents of the invention [0003] The technical problem to be solved by the present invention is: in order to overcome the above-mentioned problems, a preparation method of lercanidipine is provided. [0004] The technical solution adopted by the present invention to solve the technical problem is: a preparation method of lercanidipine. The specific steps are as follow...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D211/90
CPCC07D211/90
Inventor 李磊
Owner 李磊
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