Preparation process of clopidogre and its salt

A clopidogrel salt and a technology for clopidogrel are applied in the field of preparing clopidogrel and its pharmaceutically acceptable salts, which can solve the problems of affecting workers' health, labor consumption, energy, incomplete racemization and the like, and save operation time. and labor costs, shortening the reaction cycle, simple and time-saving effects

Inactive Publication Date: 2007-07-18
SHENZHEN SALUBRIS PHARMA CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Although the prior art proposes a method that can recycle the isomers or derivatives of the reaction intermediate substance I, this method uses thionyl chloride to reflux for 12 hours to achieve racemization. In actual production, thionyl chloride The decomposition of sulfone will produce a large amount of hydrochloric acid and sulfur dioxide gas, which will corrode the reacto

Method used

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  • Preparation process of clopidogre and its salt
  • Preparation process of clopidogre and its salt
  • Preparation process of clopidogre and its salt

Examples

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Embodiment 1

[0045] Weigh 20g of racemic o-chlorophenylglycine methyl ester hydrochloride, add 50ml of water and 150ml of dichloromethane, adjust the pH to 7-8 with sodium bicarbonate while stirring, discard the water layer after liquid separation, and use the dichloromethane layer as Wash with 50ml of water three times, dry over sodium sulfate and evaporate the solvent under reduced pressure to obtain 16g of oily substance. Dissolve the oil in 200ml of isopropanol, add 9.6g of L-tartaric acid, stir at 50°C for 0.5 hours, add seed crystals when the temperature drops to 35°C naturally, stir overnight at room temperature, cool to 20°C and stir for 4 hours, then wash the solid with suction Dry to get (+) o-chlorophenylglycine methyl ester tartrate.

[0046] The separated mother liquor was evaporated to dryness at 50°C under reduced pressure to obtain 100g of oily substance. Add 200ml of water and 200ml of dichloromethane, and adjust the pH to 7-8 with sodium bicarbonate while stirring. After...

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Abstract

The present invention provides one kind of compound with anticoagulant effect, and is especially new preparation process of clopidogrel and its pharmaceutical salt. The preparation process includes the following four steps: 1. resolving recemized methyl o-chlorophenyl glycinate to obtain (+)-methyl o-chlorophenyl glycinate and (-)-methyl o-chlorophenyl glycinate; 2. recemizing (-)-methyl o-chlorophenyl glycinate to obtain recemized (-)-methyl o-chlorophenyl glycinate; 3. repeating the steps 1 and 2; and 4. preparing clopidogrel with (+)-methyl o-chlorophenyl glycinate obtained in the step 1 and preparing the obtained clopidogrel into corresponding salt. The process of the present invention has simple path, short circulating period, low cost, high product purity, less toxic side effect and corrosion to the production apparatus.

Description

Technical field: [0001] The invention relates to a preparation method of a compound, especially a method for preparing clopidogrel and a pharmaceutically acceptable salt thereof. Background technique: [0002] Clopidogrel [Methyl S(+)-2-(2-chlorophenyl)-2-(4,5,6,7-tetrahydrothiophene[3,2-c]pyridine-5)acetate], The structural formula is as follows: [0003] [0004] Clopidogrel is a platelet aggregation inhibitor that selectively inhibits the binding of adenosine diphosphate (ADP) to its receptor and the subsequent ADP-mediated activation of the glycoprotein GPIIb / IIIa complex, thus inhibiting Platelet aggregation. Clopidogrel was first jointly developed by Japan's Daiichi Pharmaceutical and France's Sanofi (Sanofi), and was launched in the United States in 1998. [0005] At present, many patents have reported the preparation methods of clopidogrel and its salts. Patent US4847265 discusses the preparation process of (S)-(+)-clopidogrel. Patent US4529596 also reports t...

Claims

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Application Information

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IPC IPC(8): C07D495/04C07D333/00C07D211/00
Inventor 叶澄海
Owner SHENZHEN SALUBRIS PHARMA CO LTD
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