Prasugrel hydrobromide polymorph and preparation method thereof

A technology of prasugrel hydrobromide and crystal form, which is applied in the field of synthesis of antithrombotic drug prasugrel hydrobromide and its polymorphs, and can solve the problem of prasugrel hydrobromide crystal form not seen Issues such as reporting, not providing data support with good stability, and good stability

Inactive Publication Date: 2010-12-01
江苏万全特创医药生物技术有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Shandong University disclosed in Chinese patent CN200810014873.2 that the hydrobromide salt of prasugrel has good stability, but did not provide data support for good stability, so the view of good stability is not recognized
[0008] At present, there is no report on the crystal form of prasugrel hydrobromide both at home and abroad

Method used

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  • Prasugrel hydrobromide polymorph and preparation method thereof
  • Prasugrel hydrobromide polymorph and preparation method thereof
  • Prasugrel hydrobromide polymorph and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0045] Example 1: Preparation of Form A of prasugrel hydrobromide.

[0046] Dissolve 10 g of prasugrel base in 100 ml of acetone, add dropwise to the organic solution 50 ml of acetone solution dissolved with 1 times the equivalent of hydrobromic acid, as the dropwise addition proceeds, solids slowly precipitate out, and react at room temperature for 1 hour , and suction filtered to obtain 8 g of white solid, with a yield of 85%. Melting point: 133-135°C. As determined by X-ray powder diffraction, it was shown that the generated crystal form was Form A.

Embodiment 2

[0047] Example 2: Preparation of prasugrel hydrobromide crystal form B.

[0048] Take 10g of prasugrel hydrobromide crystal form A, add 50ml of ethanol, heat and stir until dissolved, reflux for half an hour, stop heating, cool naturally, stir and crystallize for 3h, filter with suction to obtain a white solid, dry in vacuum at 40° for 3h, and get Crystalline powder, melting point: 138-140°C. As determined by X-ray powder diffraction, it was shown that the generated crystal form was Form B.

Embodiment 3

[0049] Example 3: Preparation of Prasugrel Hydrobromide Form C.

[0050] Take 10g of prasugrel hydrobromide crystal form A, add 150ml of ethyl acetate, heat to reflux for 1 hour, suction filter while it is hot to obtain a white solid, dry it in vacuum at 40° for 3 hours, and obtain a crystalline powder, melting point: 163-165°C . As determined by X-ray powder diffraction, it was shown that the generated crystalline form was crystalline form C.

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Abstract

The invention mainly relates to prasugrel hydrobromide polymorph and a preparation method thereof.

Description

technical field [0001] The invention belongs to the field of medicine and chemical industry, and in particular relates to a preparation method for synthesizing antithrombotic drug prasugrel (prasugrel) hydrobromide and polymorphs thereof. Background technique [0002] The chemical name of prasugrel is 2-acetoxy-5-(a-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c ] pyridine, the structural formula is as shown in formula I. As a new generation of potent thienopyridine antiplatelet drugs, jointly developed by Sankyo Co., Ltd. and Eli Lilly and Company, it is used for the treatment of thrombosis. [0003] Prasugrel is currently marketed in the form of hydrochloride, which is a prodrug that forms an active molecule after metabolism in the body, and binds to platelet P2Y receptors to exert anti-platelet aggregation activity. Clinical studies have proved that prasugrel has a better anticoagulant effect than the current mainstream drug clopidogrel. Compared wit...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D495/04A61K31/4365A61P7/02
Inventor 丁晶晶
Owner 江苏万全特创医药生物技术有限公司
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