Blonanserin and preparation method thereof

A technology of blonanserin and compound, applied in the field of medicine

Active Publication Date: 2017-06-30
SHENZHEN WANHE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0015] However, the synthesis method of blonanserin in the prior art still needs to be improve

Method used

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  • Blonanserin and preparation method thereof
  • Blonanserin and preparation method thereof
  • Blonanserin and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0088] Example 1: Preparation of Blonanserin (#206E57)

[0089] step 1):

[0090] Add 1180ml of phenylphosphonic dichloride into the reactor, cool to below 25°C, add 900g of compound (III) into the reactor in batches at 40°C, after the addition is complete, heat the system to an internal temperature of 165-170°C, Continue the heat preservation reaction. After the raw materials are completely reacted, the temperature of the system is lowered to about 40-45°C. Slowly add the reaction solution into 13.5L of dichloromethane, stir, and then slowly add the reaction system into 13.5L of ice water, keeping the temperature below 5°C. , slowly add 10% NaOH solution dropwise to adjust the pH value to 9-10, add diatomaceous earth, filter, separate liquids, combine the organic phases, dry, remove dichloromethane, obtain about 933g dark brown solid, add 465ml absolute ethanol After refining, 631 g of an earthy yellow solid product, namely the compound of formula (II), was obtained with a...

Embodiment 2

[0093] Example 2: Preparation of Blonanserin (#206E68)

[0094] step 1):

[0095] Add 1180ml of phenylphosphonic dichloride into the reactor, cool to below 25°C, add 900g of compound (III) into the reactor in batches at 40°C, after the addition is complete, heat the system to an internal temperature of 165-170°C, Continue the heat preservation reaction. After the raw materials are completely reacted, the temperature of the system is lowered to about 40-45°C. Slowly add the reaction solution into 13.5L of dichloromethane, stir, and then slowly add the reaction system into 13.5L of ice water, keeping the temperature below 5°C. , slowly add 10% NaOH solution dropwise to adjust the pH value to 9-10, add diatomaceous earth, filter, separate liquids, combine the organic phases, dry, remove dichloromethane to obtain about 928g dark brown solid, add 900ml isopropanol After refining, 550.2 g of an earthy yellow solid, namely the compound of formula (II), was obtained with a purity g...

Embodiment 3

[0098] Embodiment 3: Preparation of blonanserin (E1)

[0099] step 1):

[0100] Add 1150ml of phenylphosphonic dichloride into the reactor, cool to below 25°C, add 900g of compound (III) into the reactor in batches at 40°C, after the addition is complete, heat the system to an internal temperature of 165-170°C, Continue the heat preservation reaction. After the reaction of the raw materials is complete, the temperature of the system is lowered to about 40-45°C. Slowly add the reaction solution into 13L of dichloroethane, stir, and then slowly add the reaction system into 13L of ice water, keeping the temperature below 5°C. Slowly add 10% NaOH solution dropwise to adjust the pH value to 9-10, add diatomaceous earth, filter, separate the liquids, combine the organic phases, dry, and remove dichloromethane to obtain about 930 g of dark brown solids, which are refined by adding 465 ml of isopropanol , to obtain 632 g of an earthy yellow solid product, namely the compound of for...

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Abstract

The invention relates to Blonanserin and a preparation method thereof. The preparation method comprises the following specific steps that firstly, the compound shown in the formula III is reacted with a chlorinating agent, namely phosphenylic oxychloride, and the compound shown in the formula II is obtained; secondly, in the presence of potassium iodide, the compound shown in the formula II is reacted with N-ethylpiperazine, and the compound shown in the formula I, namely Blonanserin, is obtained. The preparation method has the advantages shown in the description.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to an antipsychotic drug and a preparation method thereof, in particular to blonanserin and a preparation method thereof. Background technique [0002] Schizophrenia is a disorder characterized by deep cognitive and emotional dissociations that affect the most basic human behaviors, such as language, thought, perception, and self-awareness. Symptoms of the disease include a wide range, the most common being mental disorders, such as hallucinations, paranoia and delusions. [0003] According to statistics, the prevalence rate of schizophrenia in the world is 0.5% to 1.5%, and only 5% of all treated patients can finally fully recover. In addition, because schizophrenia often causes comorbidities, such as anxiety disorders, depression, or psychotropic substance abuse, according to a survey by Datamonitor, more than one-third (38%) of patients with schizophrenia suffer from at least one ...

Claims

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Application Information

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IPC IPC(8): C07D221/04
CPCC07D221/04
Inventor 汪岩峰
Owner SHENZHEN WANHE PHARMA
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