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Prasugrel salt and preparation method thereof

A technology of rapamoxate compound and compound, which is applied in carboxylate preparation, organic chemistry, etc., can solve problems such as not given more detailed evaluation, and achieve low hygroscopicity, simple operation, and good reproducibility Effect

Active Publication Date: 2015-02-25
SHANGHAI SYNCORES TECH INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the various salt forms of prasugrel currently disclosed have basically not given more detailed evaluations.

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

[0051] Dissolve 1.0 g of prasugrel free base in 20 ml of methanol, and add dropwise 100 ml of a methanol solution containing 1.04 g of pamoic acid. After dropping, stir at room temperature for 1 h to make the reaction complete. The reaction solution was left to stand at 5°C for 24 hours, filtered with suction, and vacuum-dried at 50°C for 2 hours to obtain 1.60 g of a light yellow solid with a melting point of 194.98°C.

[0052] The resulting solid was subjected to X-ray powder diffraction (XRPD) analysis (see figure 1 ), DSC-TGA thermal analysis (see figure 2 ) and DVS dynamic moisture sorption analysis (see image 3 ), infrared spectroscopy (see Figure 4 ).

Embodiment 2

[0054] Dissolve 5.0 g of prasugrel free base in 50 ml of acetone, and add dropwise 600 ml of acetone solution containing 5.20 g of pamoic acid. After dropping, stir at room temperature for 1 h to make the reaction complete. The reaction solution was allowed to stand at 5°C for 24 hours, filtered with suction, and vacuum-dried at 50°C for 2 hours to obtain 7.85 g of a light yellow solid.

Embodiment 3

[0056] Dissolve 1.0 g of prasugrel free base in 15 ml of THF, and add dropwise 100 ml of a THF solution containing 1.04 g of pamoic acid. After dropping, stir at room temperature for 1 h to make the reaction complete. The reaction solution was left to stand at 5°C for 24 hours, filtered with suction, and dried in vacuo at 50°C for 2 hours to obtain 1.20 g of a light yellow solid.

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Abstract

The invention relates to a prasugrel pamoate salt and a preparation method thereof. The prasugrel pamoate salt has a structure represented by the formula II, and has the advantages of good stability, low hygroscopicity, and high safety. Moreover, the preparation method has the advantages of simple operation and good repeatability. The provided prasugrel salt can be used as an anti-platelet drug.

Description

technical field [0001] The invention relates to platelet inhibitor Prasugrel (Prasugrel) pamoate and a preparation method thereof. Background technique [0002] The compound of the structure shown in formula I is the parent structure of the platelet inhibitor prasugrel, and its chemical name is: 2-[2-(acetyloxy)-6,7-dihydrothieno[3,2-c]pyridine- 5(4H)-yl]-1-cyclopropyl-2-(2-fluorophenyl)ethanone, jointly developed by Daiichi Sankyo and Eli Lilly and Company, was approved by the European Commission for the prevention of Atherothrombotic events in patients with acute coronary syndrome who have undergone emergency department and will undergo delayed percutaneous coronary intervention. [0003] [0004] In general, the use of pharmaceutically acceptable salts of pharmaceutical compounds, also for the platelet inhibitor prasugrel such as the compound of formula I, makes the preparation of pharmaceutically acceptable salts of such compounds particularly important. [0005] US...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D495/04C07C65/11C07C51/41
CPCC07D495/04
Inventor 许炜方干王举波武文举张席妮
Owner SHANGHAI SYNCORES TECH INC
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