Preparation method of amorphous substance of idelalisib

An amorphous and solution technology, applied in organic chemistry and other directions, can solve problems such as unfavorable industrial production, reduce production efficiency, affect yield, etc., achieve good physical and chemical stability, improve efficiency, and reduce waste water production. the effect

Inactive Publication Date: 2018-07-27
宁波爱诺医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Dichloromethane has a high solubility to Adlib, and using dichloromethane as an anti-solvent will greatly affect the yield
Such a large amount of solvent not only seriously reduces production efficiency, but also produces a large amount of waste water, which is not conducive to industrial production

Method used

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  • Preparation method of amorphous substance of idelalisib
  • Preparation method of amorphous substance of idelalisib
  • Preparation method of amorphous substance of idelalisib

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Adlib (1 g) was added to methanol (2.5 ml) and tetrahydrofuran (2.5 ml), stirred and dissolved at 50°C. The above solution was added to water (10 ml) cooled to 5°C, a white solid was precipitated under stirring, filtered, and vacuum-dried at 40-50°C to obtain 0.92 g of Adlib amorphous solid,

Embodiment 2

[0047] Adlib (1 g) was added to methanol (1 ml) and tetrahydrofuran (2 ml), stirred and dissolved at 50°C. The above solution was added to water (10 ml) cooled to 5°C, a white solid was precipitated under stirring, filtered, and vacuum-dried at 40-50°C to obtain 0.92 g of a solid, i.e. Adlib amorphous.

Embodiment 3

[0049] Adlib (1 g) was added to methanol (2 ml) and acetonitrile (2 ml), stirred and dissolved at room temperature. The above solution was added to water (20 ml) cooled to 10°C, a white solid was precipitated under stirring, filtered, and vacuum-dried at 40-50°C to obtain 0.93 g of a solid, i.e. Adlib amorphous.

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Abstract

The invention relates to a preparation method of an amorphous substance of idelalisib. The amorphous substance of idelalisib can greatly reduce usage amount of a solvent and improve industrial production efficiency, reduces generation of waste water, and further greatly reduces production cost of the product. Under an acceleration test condition at 40 +/- 2 DEG C under humidity of 75% +/- 5%, theamorphous substance maintains excellent physical and chemical stabilities.

Description

technical field [0001] The invention relates to a preparation method of an amorphous substance of Adlib. Background technique [0002] Idelalisib, the chemical name is 5-fluoro-3-phenyl-2-[(1S)-1-(9H-purin-6-ylamino)propyl]-4(3H)-quinazole Phenone, its structure is shown in formula (I): [0003] [0004] Adlib (trade name Zydelig) is a selective phosphoinositide 3-kinase delta (PI3K-delta, P110-delta) inhibitor developed by Gilead Science. On July 23, 2014, the U.S. Food and Drug Administration (FDA) approved three indications of Adlib: in combination with rituximab (Rituxan) for the treatment of relapsed chronic lymphocytic leukemia (CLL), as a monotherapy Drug therapy for relapsed follicular B-cell non-Hodgkin's lymphoma (FL) and relapsed small lymphocytic lymphoma (SLL). The FDA has accelerated approval for the latter two indications, and the patients have received at least two previous systemic treatments. [0005] Adlib is the first marketed oral, selective phosp...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D473/34
CPCC07D473/34
Inventor 张席妮熊志刚周涛朱日辉胡涛李国旺
Owner 宁波爱诺医药科技有限公司
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