Synthetic process of manidipine hydrochloride

Through a four-step process, N-hydroxyethylpiperazine was reacted with diphenylmethane, diketene, m-nitrobenzaldehyde and hydrogen chloride to successfully achieve efficient synthesis of manidipine hydrochloride and solve the complex existing process. It solves the problems of high sex, high cost and environmental pollution, and achieves industrialized production and high yield.

CN104292150AInactive Publication Date: 2015-01-21XUCHANG HENGSHENG PHARMA
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Patent Information

Application Number
CN201310302663.4
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2013-07-19
Publication Date
2015-01-21
Estimated Expiration
Not applicable · inactive patent

AI Technical Summary

Technical Problem

The existing synthesis process of manidipine hydrochloride has problems of high complexity, high cost and environmental pollution, making it difficult to achieve industrial production.

Method used

A four-step process is adopted: first, 1-diphenylmethyl-4-(2-hydroxyethyl)piperazine is obtained by reacting N-hydroxyethylpiperazine and diphenylmethane, and then reacted with diketene to generate 2-( 4-Diphenylmethyl-1-piperazinyl)ethyl acetoacetate, then reacted with m-nitrobenzaldehyde and methyl 3-aminobutenoate to obtain manidipine, which was then reacted with hydrogen chloride to form manidiprine hydrochloride The earth is flat.

Benefits of technology

The industrialized production of manidipine hydrochloride is achieved with simple process, low cost, high yield and reduced environmental pollution.

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Abstract

The invention discloses a synthetic process of manidipine hydrochloride. The method uses N-hydroxyethyl piperazine as an initial raw material, which is subjected to diketene acylation, and then condensation with m-nitrobenzaldehyde and 3-amino methyl crotonate to obtain the manidipine; and the manidipine is subjected to hydrogen chloride organic solvent salt forming to obtain the manidipine hydrochloride. The invention improves synthetic process of 1-benzhydryl-4-(2-hydroxy ethyl) piperazine; and a catalyst is introduced into the diketene acylation reaction, and the salt forming process uses a novel hydrogen chloride organic solvent method, so as to ensure product quality, improve yield and facilitate industrial production.
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