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Method for synthesizing clopidogrel hydrogen sulfate

A technology of clopidogrel hydrogen sulfate and a synthesis method, applied in directions such as organic chemistry, can solve the problems of complicated processing process, low processing efficiency, many by-products, etc., and achieve the effects of simple post-processing, convenient processing operation, and few by-products

Inactive Publication Date: 2018-10-26
安徽省金楠医疗科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The drug has remarkable clinical curative effect, few side effects, and high tolerance. It has gradually replaced aspirin and ticlopidine, and has become the first-line drug for the treatment of thrombotic diseases. Clopidogrel bisulfate has a broad market prospect and has attracted attention from the pharmaceutical industry. Widely valued, the existing processing methods have low processing efficiency, many by-products, complicated processing and high cost

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  • Method for synthesizing clopidogrel hydrogen sulfate
  • Method for synthesizing clopidogrel hydrogen sulfate
  • Method for synthesizing clopidogrel hydrogen sulfate

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Embodiment Construction

[0012] In order to make the object, technical solution and advantages of the present invention clearer, the present invention will be further described in detail below in conjunction with specific embodiments. It should be understood that the specific embodiments described here are only used to explain the present invention, not to limit the present invention.

[0013] A kind of synthetic method of clopidogrel hydrogen sulfate, comprises the steps:

[0014] S1. Synthesis of 2-(2-thiophene) ethanol p-toluenesulfonate: Put 97g p-toluenesulfonyl chloride and 180ml toluene in a three-necked flask, stir to dissolve, filter, keep warm at 15-20°C for later use, and store in a three-necked flask Put 60g of 2-thiophene ethanol, 60ml of toluene, 120g of 40% sodium hydroxide aqueous solution into the solution, stir, control the temperature at 10-20°C, add dropwise a solution of 97g of p-toluenesulfonyl chloride dissolved in 180ml of toluene, stir for 3 hours after dropping, and then heat...

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Abstract

The invention discloses a method for synthesizing clopidogrel hydrogen sulfate. The method comprises the following steps: S1, synthesizing 2-(2-thiophene) ethanol p-toluenesulfonate; S2, synthesizing(+)-L-2-chlorophenylglycine methyl ester brown oily substance; S3, synthesizing (S)-2-(2-thiopheneethylamine)(2-chlorphenyl) methyl acetate hydrochloride; and S4, synthesizing a finished product. Compared with a conventional method for synthesizing the clopidogrel hydrogen sulfate, the method has the advantages that the processing operation is more convenient, post-treatment is simple, industrialproduction is available, yield is high, few byproducts are generated, impurities can be removed more easily, materials are simple and easily available, and the cost and the price are low.

Description

technical field [0001] The invention belongs to the field of chemical pharmacy, and more specifically relates to a method for synthesizing clopidogrel hydrogen sulfate. Background technique [0002] Clopidogrel bisulfate (trade name: Plavix) is an anti-platelet aggregation drug developed by the French company Sanofi-Aventis in 1986. It is selectively coupled to platelet surface adenylate cyclase ADP receptor binds and irreversibly inhibits platelet aggregation and reduces thrombus formation in blood vessels. The drug has remarkable clinical curative effect, few side effects, and high tolerance. It has gradually replaced aspirin and ticlopidine, and has become the first-line drug for the treatment of thrombotic diseases. Clopidogrel bisulfate has a broad market prospect and has attracted attention from the pharmaceutical industry. It is widely valued that the existing processing methods have low processing efficiency, many by-products, complicated processing and high cost. ...

Claims

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Application Information

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IPC IPC(8): C07D495/04
CPCC07D495/04
Inventor 胡惠平唐中姚周章剑李杰
Owner 安徽省金楠医疗科技有限公司