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Preparation method of iloperidone

A technology of iloperidone and acetone, applied in the field of preparation of iloperidone, can solve the problems of harsh reaction conditions, low yield, low product purity and the like, and achieves a simple preparation process, high yield and high product purity. Effect

Inactive Publication Date: 2013-06-05
ANHUI YOUCARE KAIYUE PHARMA
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  • Abstract
  • Description
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  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The preparation process of iloperidone in the prior art has many synthetic routes, and there are many defects such as low yield, harsh reaction conditions, and low product purity.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0024] The present invention will be further described below in conjunction with embodiment.

[0025] ① Preparation of 2,4-difluorophenyl-4-piperidinyl ketone oxime hydrochloride

[0026] In a 2000ml dry four-necked reaction flask equipped with mechanical stirring and a thermometer, add 100g of 4-hydroxy-3-methoxyacetophenone, 10g of hydroxylamine hydrochloride, and 1000mL of absolute ethanol in sequence, and start stirring; Add 125mL of triethylamine, after dropping, heat to reflux for 15h; cool down to room temperature, filter with suction, wash with 100mL of ethanol, and dry in vacuo at 60°C to obtain 83.8g of white powder, which is designated as intermediate Ⅰ, with a yield of 79.1%.

[0027] ②. Preparation of 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole hydrochloride

[0028] In a 1000ml dry four-necked reaction flask equipped with mechanical stirring, a thermometer, and a reflux condenser, add 83g of intermediate I, 84g of solid potassium hydroxide powder, and 550ml of ...

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PUM

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Abstract

The invention relates to the technical field of drug synthesis, in particular to a preparation method of iloperidone. 95-105 grams of 4-hydroxyl-3-methoxyacetophenone, 9.5-10.5 grams of hydroxylamine hydrochloride and 950-1050 millimeters of absolute ethyl alcohol are added into a reaction vessel in sequence and mixed with the temperate controlled between 35-45 DEG C, 124-126 millimeters of triethylamine are added dropwise, and heating of backflow are conducted for 15-16 hours after the droplet addition is finished, the temperature is reduced to room temperature, reaction products are subjected to suction filtration, a filter cake is washed and dried, and white powder is obtained. The preparation method of iloperidone is simple and direct in preparation process, suitable for industrial production, high in yield coefficient, and capable of effectively shortening reaction time. Meanwhile, purification processes are simple and direct, and product purity is high.

Description

technical field [0001] The invention relates to the technical field of drug synthesis, in particular to a preparation method of iloperidone. Background technique [0002] Iloperidone (Fanapt) is mainly used for the treatment of schizophrenia. Its approval marks a new opportunity for patients with schizophrenia who are only partially responsive to many existing drug treatments to better control their symptoms. [0003] The preparation process of iloperidone in the prior art has many synthetic routes, and many defects such as low yield, harsh reaction conditions, and low product purity exist. Contents of the invention [0004] The present invention aims to overcome the technical problems in the above-mentioned prior art, and proposes a method for preparing iloperidone that has a high yield and is convenient for industrial production. [0005] The technical scheme that the present invention adopts is as follows: [0006] The preparation method of iloperidone is characteriz...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D413/04
Inventor 周如国
Owner ANHUI YOUCARE KAIYUE PHARMA
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