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Novel Aromasin crystal form and preparation process thereof

A preparation process, the technology of exemestane, is applied in the directions of steroids, organic chemistry, organic chemistry methods, etc., to achieve the effects of easy preservation, simple and reliable preparation process, and high purity

Inactive Publication Date: 2015-11-18
山东安弘制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, there are still few studies on the crystalline form of exemestane, especially the stable exemestane crystalline form

Method used

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  • Novel Aromasin crystal form and preparation process thereof
  • Novel Aromasin crystal form and preparation process thereof
  • Novel Aromasin crystal form and preparation process thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Add exemestane (10 g) and acetone (100 ml) into the reaction vessel, stir and raise the temperature to obvious reflux (45-55° C.), and reflux until the solid is completely dissolved. Maintain reflux, add petroleum ether (100ml), lower the temperature to 0-10°C, stand for crystallization for 4 hours, filter, and dry the solid at 60-70°C for 6 hours to obtain about 7.6g of the new crystal form of exemestane.

[0035] The above sample is detected, and its X-ray powder diffraction pattern is as follows: figure 1 As shown, the data are shown in Table 1.

[0036] Table 1 Example 1 Powder X-ray Diffraction Data

[0037] serial number

[0038] 4

Embodiment 2

[0040] Add exemestane (10 g) and dichloromethane (40 ml) into the reaction vessel, stir and raise the temperature to obvious reflux (35-45° C.), and reflux until the solid is completely dissolved. Maintain reflux, add petroleum ether (60ml), lower the temperature to 0-10°C, let stand for crystallization for 2 hours, filter, and dry the solid at 60-70°C for 8 hours to obtain about 8.0g of the new crystal form of exemestane.

[0041] The above sample is detected, and its X-ray powder diffraction pattern is as follows: figure 2 As shown, the data are shown in Table 2.

[0042] Table 2 Example 2 Powder X-ray Diffraction Data

[0043] serial number

Embodiment 3

[0045] Add exemestane (10 g) and dichloromethane (60 ml) into the reaction vessel, stir and raise the temperature to obvious reflux (35-45° C.), and reflux until the solid is completely dissolved. Maintain reflux, add petroleum ether (100ml), lower the temperature to 0-10°C, stand for crystallization for 3 hours, filter, and dry the solid at 60-70°C for 8 hours to obtain about 7.7g of the new crystal form of exemestane.

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Abstract

The invention relates to a novel Aromasin crystal form and a preparation process thereof. X-ray diffraction of the novel Aromasin crystal form powder has characteristic peaks at the following 2 theta angles: 10.7+ / -0.2 degrees, 11.1+ / -0.2 degrees, 13.2+ / -0.2 degrees, 14.4+ / -0.2 degrees, 15.9+ / -0.2 degrees, 16.8+ / -0.2 degrees, 18.1+ / -0.2 degrees, 19.7+ / -0.2 degrees, 21.4+ / -0.2 degrees, 23.4+ / -0.2 degrees, 27.0+ / -0.2 degrees and 29.2+ / -0.2 degrees. The novel Aromasin crystal form is stable in property, simple and convenient in preparation method, and suitable for industrial large-scale production.

Description

technical field [0001] The invention relates to a new crystal form of exemestane and a preparation process thereof, belonging to the technical field of pharmacy. Background technique [0002] Breast cancer is one of the common malignant tumors in women, and about 1 / 3 of the patients' tumor growth requires high levels of estrogen to maintain, that is, it has the characteristics of estrogen dependence. Exemestane (brand name ), which is a potent, specific, and irreversible aromatase inhibitor, which inactivates the active site of aromatase through ethyl ester, so that the level of estrogen in the circulation is rapidly and continuously reduced, thereby blocking tumors growth. The drug was launched in the United States in October 1999. It is mainly suitable for the treatment of estrogen-dependent metastatic tumors and breast cancer patients in menopausal women. It is effective when taken orally, has less toxic and side effects, and is easier to be accepted by patients. [0...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J1/00
CPCC07J1/0011C07B2200/13
Inventor 许洪飞符淙淙冯宪东赵卫良周臣生
Owner 山东安弘制药有限公司
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