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Process for producing high-purity prasugrel and acid addition salt thereof

A technology of prasugrel hydrochloride and acid addition salt, which is applied in the directions of pharmaceutical formulations, organic active ingredients, medical preparations containing active ingredients, etc., can solve the problem of not describing the method of reducing by-product OXTP and the like

Inactive Publication Date: 2009-07-01
DAIICHI SANKYO CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these patent documents do not describe methods to reduce the by-product OXTP

Method used

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  • Process for producing high-purity prasugrel and acid addition salt thereof
  • Process for producing high-purity prasugrel and acid addition salt thereof
  • Process for producing high-purity prasugrel and acid addition salt thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0115] The embodiment that uses free prasugrel to prepare high-purity prasugrel hydrochloride

[0116] To 8.00g of 2-acetoxy-5-(α-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine and 398 mg of activated clay was added to 43 g of acetone, and the resulting mixture was stirred at 32°C. The reaction solution was filtered, the residue was washed with 4.41 g of acetone, and then 1.12 g of 36% concentrated hydrochloric acid was added dropwise to the solution at 52°C over a period of 1 minute. 238 mg of Crystal B2 obtained by the method described in JP2002-145883 was added thereto as a seed crystal, and the obtained mixture was then stirred at the same temperature for one hour. Further, 1.07 g of 36% concentrated hydrochloric acid was added dropwise thereto over a period of one hour, and then the obtained mixture was stirred at 40°C for 2 hours and further stirred at 30°C for 1 hour. Precipitated crystals were collected by filtration, washed with 15.8 g o...

Embodiment 2

[0126] The embodiment that uses free prasugrel to prepare high-purity free prasugrel

[0127] To 7.00 g of Compound (I) was added 46.3 g of acetonitrile, and the resulting mixture was stirred at 40°C for 10 minutes, and then the reaction solution was cooled to -15°C. Thereto was added dropwise 29.4 g of water precooled to the same temperature over a period of 35 minutes, and then the resulting mixture was stirred at the same temperature for 30 minutes. Precipitated crystals were collected by filtration, washed with 10.5 g of a precooled acetonitrile-water mixed solvent, and dried at 45° C. under reduced pressure for 5 hours to provide 6.50 g of the title compound.

[0128] The liquid chromatography of the obtained high-purity free prasugrel is as follows: Figure 6 shown.

[0129] Figure 6 The measurement conditions in are as follows.

[0130] (Measurement Conditions) Detector: Ultraviolet Absorption Meter (Measurement Wavelength: 240nm)

[0131] Analytical column: Caden...

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PUM

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Abstract

The present invention is directed to providing prasugrel hydrochloride or the like with a reduced content of OXTP. A method for producing prasugrel hydrochloride with a reduced content of OXTP, comprising dissolving free prasugrel containing OXTP in an inert solvent and adding hydrochloric acid optionally dropwise to the solution for reaction is also provided.

Description

technical field [0001] The present invention relates to a process for the preparation of high-purity prasugrel or its acid addition salts. Background technique [0002] Compounds with the formula: [0003] [0004] Known as prasugrel. Prasugrel and its pharmaceutically acceptable salts are known to have platelet aggregation-inhibiting action and are useful as pharmaceutical active ingredients (particularly, antithrombotic or antithrombotic agents) (JP06-41139 or JP2002-145883). However, the use of prasugrel or a pharmaceutically acceptable salt thereof as a medicine requires a technique for preparing high-purity prasugrel or a pharmaceutically acceptable salt thereof. [0005] WO96 / 11203 describes a process for the preparation of prasugrel or a pharmaceutically acceptable salt thereof. Additionally, JP2002-145883 describes a process for the preparation of prasugrel hydrochloride or maleate which comprises reacting an acid with free prasugrel. However, these patent doc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D495/04A61K31/4365A61P7/02
Inventor 井上辉比古中村和良荻原昌彦宫田博之和田幸周横田尚之
Owner DAIICHI SANKYO CO LTD
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