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Preparation method of brexpiprazole, and compound used for preparing brexpiprazole

A compound and basic substance technology, applied in the field of drug synthesis, can solve problems such as long production cycle, cumbersome route, and low yield

Inactive Publication Date: 2017-07-11
连云港皓海医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This route takes 2-chloro-6-fluorobenzaldehyde as raw material to synthesize 1-(benzothiophen-4-yl)-piperazine hydrochloride through 5 steps. Long production cycle and low yield

Method used

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  • Preparation method of brexpiprazole, and compound used for preparing brexpiprazole
  • Preparation method of brexpiprazole, and compound used for preparing brexpiprazole
  • Preparation method of brexpiprazole, and compound used for preparing brexpiprazole

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Embodiment Construction

[0059] According to one aspect of the present invention, the present invention provides a compound or salt thereof represented by formula IV,

[0060]

[0061] Wherein, the salt is selected from one of hydrochloride, hydrobromide, sulfonate, methanesulfonate, p-toluenesulfonate, oxalate, phosphate or maleate.

[0062] According to one aspect of the present invention, the present invention provides a method for preparing a compound of formula IV, which comprises deprotecting the compound R of formula III in a protic polar solvent under the catalysis of Blount acid or inorganic base to obtain the compound of formula IV,

[0063]

[0064] Wherein, R in the compound of formula III is an amino protecting group;

[0065]Optionally, the amino protecting group is one of acyl and alkoxycarbonyl;

[0066] Optionally, the acyl group is selected from one of formyl, acetyl or propionyl;

[0067] Optionally, the alkoxycarbonyl group is preferably one of methoxycarbonyl, ethoxycarbon...

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PUM

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Abstract

The invention discloses a preparation method of brexpiprazole, and a compound used for preparing brexpiprazole. A compound IV reacts with a compound VIII to obtain the brexpiprazole. The preparation method has the advantages of cheap and easily available raw materials, simple synthesis technology, greenness and environmental protection, and suitableness for industrial production.

Description

technical field [0001] The invention belongs to the technical field of drug synthesis, and provides a preparation method of brepiprazole and a compound used for preparing breiprazole. Background technique [0002] Brexpiprazole (Brexpiprazole), chemical name: 7-(4-(4-(benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy)-1H-quinoline-2- Ketone, developed by Otsuka Pharmaceutical Co., Ltd., is a dopamine D2 receptor partial agonist (to improve positive and negative symptoms, cognitive impairment and depression symptoms), 5-HT2A receptor antagonist (to improve negative symptoms, cognitive dysfunction, Symptoms of depression, insomnia), Xl adrenoceptor antagonists (to improve positive symptoms of schizophrenia), serotonin uptake / reuptake inhibitors (to improve depressive symptoms); meanwhile, 5-HT1A partial agonists ( Anxiolytic and antidepressant activity) and 5-HT7 antagonist. It was approved by the US FDA in 20150711 for the adjuvant treatment of schizophrenia and severe depression....

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D215/22C07D487/10C07D409/12
CPCC07D215/22C07D409/12C07D487/10Y02P20/55
Inventor 许恒皓李娇娇毕震宇
Owner 连云港皓海医药科技有限公司
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