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Preparing method for brexpiprazole

A technology for epipiprazole and compound, applied in the field of chemical drug synthesis, can solve the problems of unfavorable industrial preparation of epipiprazole and high cost, and achieve the effects of avoiding metal catalyst, reducing reaction cost and high synthesis yield

Inactive Publication Date: 2016-04-06
NANJING CORE TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0027] (2) In the patent CN103717587, this route has been modified, and the reactant for preparing compound 6 is changed from compound 5 piperazine to monoprotected piperazine (R is a protecting group, such as Boc, etc.), so that side reactions in the reaction Correspondingly reduced, but this route just cost is still higher, is unfavorable for industrialized preparation ebiprazole

Method used

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  • Preparing method for brexpiprazole
  • Preparing method for brexpiprazole
  • Preparing method for brexpiprazole

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] (1) Preparation of compound shown in formula D

[0054]

[0055] In a 5000mL four-neck round bottom flask, add 400g of the compound shown in formula B (2.5mol), add NMP (nitromethylpyrrolidone) 1600mL, then add 493g of the compound shown in formula C (2.7mol), 489g of DIPEA (N, N-diisopropylethylamine) (3.75mol, 1.5eq), then heat the reaction system to 100°C, and react at this temperature for 12 hours, then cool the reaction system to 5°C, add water and acetone mixture 2000mL (water: acetone = 2:1), and stirred at 5°C for 30 minutes, a light yellow solid precipitated, filtered out the solid, and washed with 500mL of water, and then the obtained solid was air-dried at 50°C to obtain a light yellow solid 805.3 g, yield 97.3%.

[0056] (2) Preparation of compound shown in formula F

[0057]

[0058] In a 10L three-necked flask, add 1.0kg of the compound represented by formula D (3.08mol), 1.7kg of potassium carbonate (12.32mol), 4L of DMF (N,N-dimethylformamide), a...

Embodiment 2

[0076] (1) Preparation of compound shown in formula D

[0077]

[0078] In a 5000mL four-neck round bottom flask, add 400g of the compound shown in Formula B (2.5mol), add 1600mL of dimethyl sulfoxide, and then add 493g of the compound shown in Formula C (2.7mol), 570.5g of DBU (1,8 -diazabicycloundec-7-ene) (3.75mol, 1.5eq), then heated the reaction system to 90°C, and reacted at this temperature for 10 hours, then cooled the reaction system to 5°C, added Mix 2000mL of water and acetone (water: acetone = 2:1), and stir at 0°C for 30 minutes, a light yellow solid precipitates, filter out the solid, wash it with 500mL of water, and blow the resulting solid at 50°C After drying, 787.9 g of light yellow solid was obtained, and the yield was 95.2%.

[0079] (2) Preparation of compound shown in formula F

[0080]

[0081] In a 10L three-necked flask, add 1.0kg of the compound represented by formula D (3.08mol), 492.8g of sodium hydroxide (12.32mol), and 4L of nitrogen methy...

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Abstract

The invention belongs to the technical field of chemical drug synthesis and particularly relates to a preparing method for brexpiprazole. According to the preparing method, crystalline brexpiprazole is prepared through five steps. The preparing method has the advantages that the synthetic yield is high, operation is simple, purification is easy, and the end product is stable. In addition, a metal catalyst is effectively avoided, and the number of reaction steps is greatly reduced, so that the reaction difficulty is lowered, post-treatment is simplified, the yield is increased, the reaction cost is greatly reduced, and thus industrialized mass production is facilitated.

Description

technical field [0001] The invention belongs to the technical field of chemical drug synthesis, and in particular relates to a preparation method of ebiprazole. Background technique [0002] Brexpiprazole (Brexpiprazole), the chemical name is 7-(4-(4-(benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy)-1H-quinoline-2- Ketones, the structural formula is as follows: [0003] [0004] Clinical trial indications are schizophrenia, major depressive disorder, attention deficit movement disorder, post-traumatic stress disorder, and restless dementia. [0005] Schizophrenia (English: Schizophrenia, translated into schizophrenia in Taiwan in 2014) is a serious mental illness, the symptoms of which are the breakdown of thinking patterns and emotions. Common symptoms include hallucinations, delusions, and gibberish. In severe cases, there will be a tendency to self-destruct and hurt others, and social or occupational functioning will deteriorate. Patients usually show initial symptoms i...

Claims

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Application Information

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IPC IPC(8): C07D409/12
CPCC07D409/12
Inventor 王雪根何凌云余洋金皓杰郭莉芹
Owner NANJING CORE TECH CO LTD
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