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Synthesis method of clopidogrel hydrogen sulfate

A technology of clopidogrel hydrogen sulfate and synthetic method, which is applied in the field of synthesis of clopidogrel hydrogen sulfate, and achieves the effects of good quality, broad market prospect and mild reaction conditions

Inactive Publication Date: 2017-11-24
JIANGSU HI STONE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] The technical problem mainly solved by the present invention is to provide a synthetic method of clopidogrel bisulfate, which can solve the shortcomings of the existing synthetic methods

Method used

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  • Synthesis method of clopidogrel hydrogen sulfate
  • Synthesis method of clopidogrel hydrogen sulfate
  • Synthesis method of clopidogrel hydrogen sulfate

Examples

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Embodiment 1

[0062] Add 400~500ml of acetone to the reaction vessel, then add 180~200g of 2-(2-chlorophenyl)acetic acid, stir evenly, keep the constant temperature at 20~30°C, then slowly add 120~150ml of thionyl chloride dropwise , heated to 40-50°C, and stirred at a rate of 50-150r / min for 1h. After the reaction was terminated, the solvent was evaporated under reduced pressure to obtain crude 2-(2-chlorophenyl)acetyl chloride.

[0063] Add the above crude 2-(2-chlorophenyl)acetyl chloride into the reaction vessel, heat it to 50-60°C, and slowly add 60-65ml of dried anhydrous Br 2 , After dropping, heat to 60~70°C and reflux for 2~3h to obtain crude 2-bromo-2-(2-chlorophenyl)acetyl chloride.

[0064] Add the above-mentioned 2-bromo-2-(2-chlorophenyl)acetyl chloride into the reaction vessel, then slowly add 500-600ml of methanol dropwise at a rate of 10-15ml / min, and let stand for 30-60min until the reaction is gentle. Then add triethylamine dropwise at a rate of 5-10ml / min, after droppin...

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Abstract

The invention discloses a synthesis method of clopidogrel hydrogen sulfate. The synthesis method takes o-phenylphthalic chloroacetic acid and 4,5,6,7tetrahydrothiophene[3,2-c] as raw materials and comprises the following steps: (1) carrying out acylation reaction; (2) carrying out bromination reaction; (3) carrying out esterification reaction; (4) preparing a clopidogrel base crude product; (5) extracting clopidogrel base; (5) carrying out racemic racemate reductionresolution; (7) preparing the clopidogrel hydrogen sulfate. According to the synthesis method of the clopidogrel hydrogen sulfate, disclosed by the invention, reasonable raw material selection and process route design are carried out, so that on one hand, a process flow is simplified and synthesis operation is easy to realize; on the other hand, reaction conditions are reduced, the reaction conditions are moderate and the method is easily smoothly carried out; the obtained finished product clopidogrel hydrogen sulfate has high yield and good quality; industrial production is easy to realize and a market prospect is wide.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical synthesis, in particular to a synthesis method of clopidogrel bisulfate. Background technique [0002] Cardiovascular and cerebrovascular thrombotic disease is a major disease that seriously affects human health, but inhibiting platelet aggregation is an effective way to treat this disease. Clopidogrel is a platelet aggregation inhibitor, it can selectively inhibit the binding of ADP to platelet receptors, and then inhibit the activation of ADP and glycoprotein GPIIb / IIIa complex, thereby inhibiting the aggregation of platelets, and can also inhibit the non-ADP-induced platelet aggregation without affecting phosphodiesterase activity. Clopidogrel affects the lifespan of platelets by irreversibly altering the platelet ADP receptor. As an acetic acid derivative of ticlopidine, clopidogrel has the advantages of strong curative effect, low cost, and small side effects. In-stent restenosis an...

Claims

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Application Information

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IPC IPC(8): C07D495/04
CPCC07D495/04C07B2200/07
Inventor 王多平卫耿虎史加桂杨宇
Owner JIANGSU HI STONE PHARMA
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