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Crystal form I of clopidogrel hydrochloride and preparation method and application thereof

A technology of clopidogrel hydrochloride and clopidogrel, which is applied in the field of medicine and can solve problems such as poor reproducibility, low yield, and commercial scale-up

Active Publication Date: 2013-04-10
TIANJIN CHASE SUN PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Its preparation process has the characteristics of long reaction time (up to 16 hours), low yield (65%-85%), commercial amplification and poor reproducibility

Method used

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  • Crystal form I of clopidogrel hydrochloride and preparation method and application thereof
  • Crystal form I of clopidogrel hydrochloride and preparation method and application thereof
  • Crystal form I of clopidogrel hydrochloride and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Example 1: Clopidogrel hydrochloride crystal form Ⅰ

[0048] Weigh 20.0g of clopidogrel, add it into 60mL of ethyl acetate, stir, dissolve all and mix evenly, cool to 5°C, add 5mol / L hydrochloric acid ethyl acetate solution dropwise, until no precipitation occurs, about 5ml, Maintain the temperature and stir for 4 hours, filter, and vacuum-dry for about 24 hours to obtain a white crystalline powder.

Embodiment 2

[0049] Example 2: Clopidogrel hydrochloride crystal form Ⅰ

[0050] Weigh 20.0g of clopidogrel, add it into 150mL of ethyl acetate, stir to dissolve all and mix evenly, cool to 5°C, add 5mol / L diethyl ether solution of hydrochloride dropwise until no precipitation occurs, about 5ml, keep the temperature Stir for 4 hours, filter, and vacuum dry for about 24 hours to obtain a white crystalline powder.

Embodiment 3

[0051] Example 3: Clopidogrel hydrochloride crystal form Ⅰ

[0052]Weigh 20.0g of clopidogrel, add it to 240mL of ethyl acetate, stir to dissolve all and mix evenly, cool to 5°C, add 5mol / L tert-butyl methyl ether hydrochloride solution dropwise until no precipitation occurs, about 5ml , kept stirring at the temperature for 4 hours, filtered, and dried in vacuum for about 24 hours to obtain a white crystalline powder.

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PUM

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Abstract

The invention relates to the technical field of medicine, in particular to clopidogrel hydrochloride or a crystal form I of the clopidogrel hydrochloride and a preparation method thereof, a medicinal composition containing the crystal form I and application of the crystal form I in preparation of anti-platelet aggregation medicines. The crystal form I of the clopidogrel hydrochloride has peaks at12.960 DEG, 19.860 DEG, 23.020 DEG, 24.920 DEG and 25.340 DEG represented by a 2theta angle in X-ray powder diffraction by using Cu-Ka radiation.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to clopidogrel hydrochloride or clopidogrel hydrochloride crystal form I, a preparation method thereof, a pharmaceutical composition containing it and its use in the manufacture of anti-platelet aggregation drugs. Background technique [0002] Clopidogrel [2-(2-chlorophenyl)-2-(6,7-dihydrothieno[3,2-c]pyridin-5-yl)methyl acetate bisulfate] is a platelet aggregation Inhibitors. [0003] Since 2005, clopidogrel as an anticoagulant drug has been used clinically for the treatment and prevention of myocardial infarction and has been widely used in clinical heart disease patients. Taking clopidogrel can significantly reduce the incidence of myocardial infarction. Clopidogrel has become a The top three pharmaceuticals in terms of global sales, with annual sales exceeding US$6 billion. [0004] Clopidogrel can be used to prevent and treat myocardial infarction, ischemic cerebral thrombos...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D495/04A61K31/4365A61P9/10
Inventor 姚小青孙长海董凯张存彦李增辉
Owner TIANJIN CHASE SUN PHARM CO LTD
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