Regadenoson crystal form and preparation method thereof

A technology of regadesone and crystal form, applied in the field of medicinal chemistry, can solve problems such as harshness, compound decomposition, difficulty in repeating and amplifying

Inactive Publication Date: 2015-11-25
SHANGHAI ZIYUAN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the method described in this patent is too complicated and harsh to repeat and scale up, and it needs to be heated to a high temperature of 150°C, which can easily cause the compound to decompose

Method used

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  • Regadenoson crystal form and preparation method thereof
  • Regadenoson crystal form and preparation method thereof
  • Regadenoson crystal form and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Embodiment 1: Preparation of Regardson crystalline form E

[0040] Dissolve 1 g of regadepine in 10 mL of DMF, add 10 mL of dichloromethane, and concentrate under reduced pressure at 50° C. to obtain 1 g of regadepine crystal form E with a content of 92%. The X-ray powder diffraction pattern and the infrared spectrogram of this crystal form are respectively as follows Figure 5 , Figure 6 shown.

Embodiment 2

[0041] Embodiment 2: Preparation of Regardson crystalline form E

[0042] Dissolve 1 g of regadepine in 10 mL of DMF, add 10 mL of tetrahydrofuran, and concentrate under reduced pressure at 50° C. to obtain 1 g of regadepine crystal form E with a content of 91%. The X-ray powder diffraction and infrared spectrum results of this crystal form are consistent with Example 1.

Embodiment 3

[0043] Embodiment 3: Preparation of Regardson crystalline form E

[0044] Dissolve 1 g of regadepine in 10 mL of DMF, add 5 mL of ethanol, and concentrate under reduced pressure at 50° C. to obtain 1 g of regadepine crystal form E with a content of 91%. The X-ray powder diffraction result and infrared spectrum of this crystal form are consistent with Example 1.

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Abstract

The present invention relates to the field of pharmaceutical chemistry, and discloses a new regadenoson crystal form, ie., regadenoson crystal form E, and a preparation method of the new regadenoson crystal form. According to the present invention, the regadenoson crystal form E has excellent performances in the field of radionuclide myocardial perfusion imaging, has characteristics of weak toxicity and good storage stability, and can be used for preparing drugs for radionuclide myocardial perfusion imaging stress agents.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a new crystal form E of regadesone and a preparation method thereof. Background technique [0002] Regardson, chemical name (1-{9[4S,2R,3R,5R]-3,4-dihydroxy-5-(hydroxymethyl)oxol-2-yl]-6-amino Purin-2-yl}pyrazol-4-yl)-N-methylformamide, the structural formula is as follows: [0003] [0004] The U.S. Patent Publication No. US6403567B1 disclosed Regadeson, its preparation method and use for the first time. Regadeson is a highly selective adenosine A2A receptor agonist, which is used as a stress agent drug for radionuclide cardiac perfusion imaging. It has been clinically used in the United States as a cardiac vasodilator for cardiac imaging. [0005] Drug polymorphism is a common phenomenon in drug research and development, and is an important factor affecting drug quality. Polymorphism refers to the phenomenon that the same compound can form two or more molecular spatial ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H19/167C07H1/06A61K31/7076A61P9/08
Inventor 刘伟张志刚鲍芹
Owner SHANGHAI ZIYUAN PHARMA
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