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Prasugrel salt and preparation method thereof

A thunder salt compound, a Chinese-style technology, applied in the field of platelet inhibitor prasugrel salt and its preparation, can solve the problems of properties such as solubility, heat stability, moisture absorption, no detailed evaluation, and no obvious medicinal properties Advantages and other issues, to achieve the effect of good water solubility, good thermal stability and low hygroscopicity

Active Publication Date: 2011-03-16
CHINA RESOURCES SAIKE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Although a large number of prasugrel salts have been disclosed in many patents, no detailed evaluation has been given on the properties of various salts such as solubility, thermal stability, moisture absorption, etc. After our research on the disclosed salts, except Sankyo Except for the hydrochloride and maleate, other various salts have no obvious advantages in medicinal properties, but the above-mentioned properties are very important for pharmaceutically acceptable salts, so continue to search for new types of pharmaceutically acceptable salts. Acceptable Salt Still Matters

Method used

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  • Prasugrel salt and preparation method thereof
  • Prasugrel salt and preparation method thereof
  • Prasugrel salt and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1: Prasugrel cystine salt

[0035] Dissolve 3.73g of prasugrel base in an appropriate amount of acetone / methanol (volume ratio 1 / 1), add dropwise the aforementioned organic solution of 2.52g of cystine, heat to reflux for 2h, filter after cooling to obtain prasugrel cystine salt Crude. Recrystallize from ethyl acetate to obtain 4.9 g of fine prasugrel cystine salt. Melting point: 250°C (carbonization).

Embodiment 2

[0036] Example 2: Prasugrel Phenylalanine Salt

[0037] Dissolve 3.73g of prasugrel base in an appropriate amount of acetone / methanol (volume ratio 1 / 1), add dropwise the aforementioned organic solution of 1.73g of phenylalanine, heat to reflux for 2h, filter after cooling to obtain prasugrel phenylalanine Crude acid salt. Recrystallized from ethyl acetate to obtain 4.19 g of fine prasugrel phenylalanine salt. Melting point: 250°C (carbonization).

Embodiment 3

[0038] Example 3: Prasugrel Threonine Salt

[0039] Dissolve 3.73g of prasugrel base in an appropriate amount of acetone / methanol (volume ratio 1 / 1), add dropwise the aforementioned organic solution of 1.25g of threonine, heat to reflux for 2h, filter after cooling to obtain prasugrel threonine salt Crude. Recrystallized from ethyl acetate to obtain 3.44 g of fine prasugrel threonine salt. Melting point: 250°C (carbonization).

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PUM

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Abstract

The invention relates to Prasugrel salt and a preparation method thereof. The Prasugrel salt compound has a structure as formula II, wherein HA is acid, including cystine, asparagine, phenylalanine, threonine, tyrosine, glutamine, serine, methionine, tryptophane, valine, leucine, isoleucine, glycine, alanine and proline.

Description

technical field [0001] The invention relates to a platelet inhibitor Prasugrel (Prasugrel) salt and a preparation method thereof. Background technique [0002] The compound with the structure shown in formula I is the parent structure of the oral anti-platelet drug Prasugrel (prasugrel base) (referred to as prasugrel base in this patent), and was jointly developed by the American pharmaceutical company Eli Lilly and Japan's Daiichi Pharmaceutical Sanko. US Patent No. 5,288,726 discloses several new tetrahydrothienopyridine compounds including compounds of formula I, which have good anticoagulant and antithrombotic effects, and can be used for the treatment of related diseases such as heart disease. [0003] [0004] Typically, pharmaceutically acceptable salts of pharmaceutical compounds are used. The same is true for antiplatelet drugs such as compounds of formula I, which makes the preparation of pharmaceutically acceptable salts of such compounds particularly importan...

Claims

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Application Information

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IPC IPC(8): C07D495/04
Inventor 艾鑫淼邹江杨琰
Owner CHINA RESOURCES SAIKE PHARMA
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