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Crystal form B of blonanserin and preparing method thereof

A technology of crystal form and ethylpiperazine, which is applied in the field of blonanserin crystal form B and its preparation, can solve problems such as unsatisfactory stability, and achieve good development and utilization prospects, good stability, and difficulty in crystal transformation. Effect

Active Publication Date: 2010-06-23
ZHEJIANG HUAHAI PHARMACEUTICAL CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] According to existing literature, blonanserin oral preparations use 0.1mol / L hydrochloric acid as the eluent, however, crystal form A is slightly soluble in 0.1mol / L hydrochloric acid, and its solubility is only 1mg / 160ml, and its stability is also low. not ideal

Method used

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  • Crystal form B of blonanserin and preparing method thereof
  • Crystal form B of blonanserin and preparing method thereof
  • Crystal form B of blonanserin and preparing method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0026] Add 1 g of blonanserin to 10 ml of ethanol and heat to dissolve at 78°C, then cool to room temperature while stirring, and filter after 2 hours. Dry at 60°C. The product was obtained 0.9 g. The product is proved by X-ray powder diffraction to be the crystal form B of 2-ethylpiperazine-4-(4-fluorobenzene)-5,6,7,8,9,10-hexahydrocyclooctanopyridine, It exhibits an X-ray powder diffraction pattern with characteristic peaks represented at about 7.74, 15.6, 19.1 and 31.64 in 2θ° as figure 2 shown. The melting point of the crystal form B was measured to be 125-127°C.

Embodiment 2

[0028] Add 7.4 g of blonanserin to 100 ml of ethanol and heat to dissolve at 78°C, then cool to room temperature while stirring, and filter after 2 hours. Dry at 60°C. 6.5 g of product were obtained. The product was proved to be crystal form B of 2-ethylpiperazine-4-(4-fluorobenzene)-5,6,7,8,9,10-hexahydrocyclooctanopyridine by X-ray powder diffraction. The melting point of the crystal form B was measured to be 125-126°C.

Embodiment 3

[0030] Add 82.8 g of blonanserin to 500 ml of ethanol and heat to dissolve at 78°C, then cool to room temperature while stirring, and filter after 2 hours. Dry at 60°C. 72 g of product were obtained. The product was proved to be crystal form B of 2-ethylpiperazine-4-(4-fluorobenzene)-5,6,7,8,9,10-hexahydrocyclooctanopyridine by X-ray powder diffraction. The melting point of the crystal form B was measured to be 125-126°C.

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Abstract

The invention provides a crystal form B of medicament 2-ethylpiperazine-4-(4-fluorobenzene)-5,6,7,8,9,10-hexahydro cyclooctane pyridine, which is characterized in that powder diffraction occurs in the positions of approximately 7.74+ / -0.2, 15.6+ / -0.2, 19.1+ / -0.2 and 31.64+ / -0.2 of a reflecting angle 2 theta through X-ray. The invention also provides a preparing method of the crystal form B, which is characterized by comprising the following steps of: ensuring that the medicament 2-ethylpiperazine-4-(4-fluorobenzene)-5,6,7,8,9,10-hexahydro cyclooctane pyridine is dissolved in ethanol by heating, and then obtaining the crystal form B through recrystallization.

Description

technical field [0001] The present invention relates to the crystal form B of 2-ethylpiperazine-4-(4-fluorobenzene)-5,6,7,8,9,10-hexahydrocyclooctanopyridine (Blonanserin, Blonanserin) and its preparation method. Background technique [0002] The general name of 2-ethylpiperazine-4-(4-fluorobenzene)-5,6,7,8,9,10-hexahydrocyclooctanopyridine of the following structural formula is Blonanserin (Blonanserin), Mainly used for the treatment of atypical psychosis. [0003] [0004] Blonanserin [0005] Both EP385237 and JP4099768A report the synthesis method of blonanserin, but do not discuss the problem of crystal form. In the literature Analytical Sciences, 2002, 18: 1289-1290, single crystal diffraction of blonanserin in chloroform was mentioned, which is also the only report on the crystal form of blonanserin. We have obtained the crystal according to the above-mentioned literature method, and its crystal form is proved to be crystal form A through X-ray powder diffracti...

Claims

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Application Information

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IPC IPC(8): C07D221/04A61K31/496A61P25/18
Inventor 王俊芳王小妹王哲烽时惠麟王小梅隋强
Owner ZHEJIANG HUAHAI PHARMACEUTICAL CO LTD
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