Production technique of clopidogrel hydrogen sulfate

A technology of clopidogrel hydrogen sulfate and production process, applied in the field of production technology of clopidogrel hydrogen sulfate, can solve the problems of difficult separation of solvent, complicated process, increased drug cost, etc., and achieves improved drug safety, simple process, and reduced cost The effect of the synthetic steps

Inactive Publication Date: 2015-04-29
ANHUI YOUCARE KAIYUE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The synthesis process of clopidogrel bisulfate is complicated now, and the solvent etc. are not easy to separate during the synthesis process, resulting in an increase in the cost of the drug

Method used

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  • Production technique of clopidogrel hydrogen sulfate
  • Production technique of clopidogrel hydrogen sulfate
  • Production technique of clopidogrel hydrogen sulfate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0017] Step 1: Preparation of Amine Hydrochloride

[0018] 1.1 Preparation of o-chlorophenylglycine methyl ester

[0019] Material name Feeding amount Reagent specifications Material action 2-chlorophenylglycine methyl ester tartrate 4kg Internal Control Standards Starting material, obtain o-chlorophenylglycine methyl ester after desalination Dichloromethane 12L+4L*2=20L (26.5kg) industry Reaction solvent, dissolve o-chlorophenylglycine methyl ester ammonia 4kg industry Adjust pH value, dissolve o-chlorophenylglycine methyl ester in alkaline environment purified water 16L self made Dissolving o-chlorophenylglycine methyl ester tartrate Anhydrous Sodium Sulfate 2.7kg industry desiccant

[0020] Table 1

[0021] Table 1 is the raw material and the effect of raw material that o-chlorophenylglycine methyl ester is prepared.

[0022] Process Description:

[0023] Reaction: Add 4kg of o-chlorophenylglycine m...

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Abstract

The invention relates to a production technique of clopidogrel hydrogen sulfate, which comprises the following steps: (1) preparation of amide hydrochloride, (2) preparation of levo-camphorsulfonate, (3) preparation of clopidogrel hydrogen sulfate crude product and (4) preparation of I-type clopidogrel hydrogen sulfate. The technique is simple, reduces the synthesis steps, lowers the consumption of toxic solvents, enhances the drug safety, facilitates the recovery and treatment of the waste liquid and lowers the production cost. The purity of the clopidogrel hydrogen sulfate obtained by the method is high, and the yield is 6.5% higher than other methods.

Description

technical field [0001] The invention belongs to the field of chemical synthesis, in particular to a production process of clopidogrel bisulfate. Background technique [0002] Clopidogrel bisulfate is a new type of anti-platelet aggregation drug similar to ticlopyridine, which was successfully developed by Sanofi-Santa Delabourg, France. It is suitable for the prevention and treatment of heart, brain and other diseases caused by high platelet aggregation. Arterial circulation disorders, such as recent stroke, myocardial infarction, and patients with confirmed peripheral arterial disease. At present, it has been widely used in many countries including the United States, Europe and China. This product inhibits platelet activation by inhibiting the adenosine diphosphate (ADP) pathway, thereby inhibiting platelet aggregation. Because clopidogrel bisulfate takes several days to reach effective blood levels, it is not indicated for emergency treatment. After stopping this produc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D495/04
CPCC07D495/04
Inventor 周如国
Owner ANHUI YOUCARE KAIYUE PHARMA
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