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Method for refining brexpiprazole

An epipiprazole, refined technology, applied in the field of medicinal chemistry, can solve the problems of high impurity content, low product purity, low yield and the like, and achieves the effects of high purity, reduced impurity content, and simple operation

Inactive Publication Date: 2018-03-06
TIANJIN HANKANG PHARMA BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The inventor of the present application has studied the refinement method of the crude product of ebiprazole in the prior art, and found that the method recorded in the prior art still has problems such as very complicated operation process, low product purity, high impurity content, and low yield. Therefore, this There is an urgent need for a good refinement method to refine ebiprazole

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] (1) Put 5.0 g of crude ebiprazole into a single-necked bottle, add 1000 ml of diethyl ether and acetone mixture (diethyl ether: acetone = 1: 2.5), stir and dissolve at 45°C, and stir and analyze at 20°C. Crystal 2 hours;

[0016] (2) The precipitated ebiprazole crystals were collected by filtration, washed with 80 ml of ethanol pure aqueous solution (ethanol: pure water=1: 3) mixed solution, and dried in an oven at 30° C. to obtain 4.5 g of ebiprazole crystals , yield 90%, purity (HPLC) 99.2%.

Embodiment 2

[0018] (1) Put 5.0 g of crude ebiprazole into a one-mouth bottle, add 1250 ml of diethyl ether and acetone mixture (diethyl ether: acetone = 1:1), stir to dissolve at 40°C, and stir to crystallize at 25°C 4 hours;

[0019] (2) The precipitated ebiprazole crystals were collected by filtration, washed with 100ml ethanol pure aqueous solution (ethanol: pure water=1: 4) mixture and dried in an oven at 30°C to obtain 4.6g ebiprazole crystals , yield 92%, purity (HPLC) 99.4%.

Embodiment 3

[0021] (1) Put 5.0 g of the crude product of ebiprazole into a single-mouth bottle, add 1000 ml of isopropyl ether and acetone mixture (isopropyl ether: acetone = 1: 3), stir and dissolve at 35° C. Stir and crystallize at ℃ for 5 hours;

[0022] 2) The precipitated ebiprazole crystals were collected by filtration, washed with 120ml ethanol pure aqueous solution (ethanol: pure water=1: 3) mixed solution and dried in an oven at 30°C to obtain 4.55g ebiprazole crystals, Yield 91%, purity (HPLC) 99.2%.

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PUM

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Abstract

The invention belongs to the field of medicinal chemistry, and relates to a refined method of ebiprazole, which involves stirring and crystallizing crude ebiprazole with a mixture of ethers and ketones; collecting by filtration, washing, and vacuum drying to obtain pure ebiprazole The yield of prarazole crystals is more than 90%, and the purity (HPLC) reaches 99.4%, which reduces the impurities to about 0.1%.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to a refined method for ebiprazole. Background technique [0002] The chemical name of brexpiprazole is 7-(4-(4-(benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy)-1 H -Quinolin-2-one, a serotonin-dopamine activity modulator (SDAM), has partial dopamine D2 receptor agonism and 5-HT1A receptor agonism, and also has 5-HT2A receptor antagonism, developed by Japan Originally developed by Otsuka Pharmaceutical Co., Ltd., jointly developed by Otsuka Pharmaceutical and Lundbeck. [0003] The preparation method of ebiprazole is disclosed in the prior art, wherein in the example of CN105461704A, it is loaded that a mixed solution of methanol and water is used to refine the crude product of ebiprazole. [0004] The inventor of the present application has studied the refinement method of the crude product of ebiprazole in the prior art, and found that the method recorded in the pri...

Claims

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Application Information

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IPC IPC(8): C07D409/12
CPCC07D409/12
Inventor 严洁李轩
Owner TIANJIN HANKANG PHARMA BIOTECH
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