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Right-handed indobufen and use for preparing medicament

A technology for dextroindobufen and antiplatelet drugs, which is applied in the field of dextroindobufen and its preparation, and can solve the problems of preparation of a single dextrorotatory optical isomer and the lack of attention to its medicinal value.

Inactive Publication Date: 2008-09-24
FUKANGREN BIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The currently used indobufen is a racemate, and the preparation and medicinal value of its single dextrorotatory optical isomer have not been paid attention to. Its chemical name is: S-(+)-4-[1,3- Dihydro-1-oxo-(2H)-isoindol-2-yl]-α-ethylphenylacetic acid, as shown in formula I:

Method used

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  • Right-handed indobufen and use for preparing medicament
  • Right-handed indobufen and use for preparing medicament
  • Right-handed indobufen and use for preparing medicament

Examples

Experimental program
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Effect test

Embodiment 1

[0012] The preparation of embodiment 1 dextroindobufen

[0013] Add 50 grams of indobufen, 21.5 grams of (S)-(-)-α-phenethylamine, and 500 ml of ethanol into a 1L reaction bottle, heat to dissolve completely, leave at room temperature overnight for crystallization, filter, wash with ethanol, The resulting solid was recrystallized twice from ethanol, then treated with 2N hydrochloric acid, filtered and washed with water to obtain 11.8 g of dextroindobufen. [α] D =+82.3° (C=1.0, DMF), mp 196-198°C.

Embodiment 2

[0014] The preparation of embodiment 2 dextroindobufen

[0015] Add 50 grams of indobufen, 30.4 grams of (S)-(-)-α-naphthylethylamine, and 500 ml of ethanol into a 1L reaction bottle, heat to dissolve completely, leave at room temperature overnight for crystallization, filter, wash with ethanol, The resulting solid was recrystallized twice from ethanol, then treated with 2N hydrochloric acid, filtered and washed with water to obtain 11.4 g of dexindobufen. [α] D =+81.9° (C=1.0, DMF), mp 196-198°C.

Embodiment 3

[0016] The preparation of embodiment 3 dextroindobufen tablet

[0017] Take 200g of dextroindobufen, add 30g of starch and 15g of lactose, mix well, use 75% ethanol solution to make soft material, granulate with 20 mesh sieve, dry at 60°C, granulate with 20 mesh sieve after drying, add After 3.5 g of sodium carboxymethyl starch and 1.5 g of magnesium stearate are mixed evenly, a No. 9 punch die is used to adjust the tablet weight to 0.25 g / tablet, and the tablets are compressed to obtain final product. The assay result content is 100.2%, and after 6 months of long-term sample retention, it still remains stable. There was no significant change in the detection indicators from the 0 day.

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Abstract

The present invention provides dextral indobufen or acceptable salt in pharmacy, which has a structure as shown in formula I. The compound can be used as an anti-platelet drug.

Description

technical field [0001] The invention relates to an anti-platelet dextroindobufen and a preparation method thereof. Background technique [0002] Cardiovascular and cerebrovascular diseases are the most serious diseases that threaten human health in the world today, and their incidence has surpassed tumors and ranked first. Thrombosis caused by platelet aggregation is an important cause of cardiovascular and cerebrovascular diseases, and the morbidity and mortality account for a considerable proportion of middle-aged and elderly people. With the understanding of the process of thrombosis and the study of the pathogenesis of thrombotic diseases, people are more Focus on prevention of thrombosis and treatment of reinfarction after thrombolysis or percutaneous coronary angioplasty (PICA). [0003] Indobufen is a new generation of powerful anti-platelet aggregation drugs, it can selectively act on circulating platelets, block thrombus formation, and exert an anti-platelet aggreg...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D209/34A61K31/404A61P7/02
Inventor 姚勇敢
Owner FUKANGREN BIO PHARMA
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