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Method for preparing blonanserin

A technology for blonanserin and compounds, which is applied to chemical instruments and methods, medical preparations containing active ingredients, pharmaceutical formulations, etc., can solve problems such as unfavorable industrial production, inconvenient post-processing and purification, and difficulty in stirring, and achieves low cost. , high purity, strong controllable effect

Inactive Publication Date: 2011-01-26
BEIJING D VENTUREPHARM TECH DEV
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Problems solved by technology

The disadvantage of the above method is that the acquisition of blonanserin requires a high-temperature reaction above 170°C, which is difficult to achieve in industry. In addition, the above-mentioned reaction is carried out under a solvent-free high-temperature melting condition, which is not only difficult to stir, but also requires post-processing. Purification brings great inconvenience
In view of the fact that there are many factors that are not conducive to industrial production in this step reaction process, and the yield is low, and based on the pharmaceutical value and good market prospect of blonanserin, it is necessary to find a synthetic method with good yield and strong controllability. An effective method for the compound of formula (I) is imperative

Method used

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  • Method for preparing blonanserin
  • Method for preparing blonanserin
  • Method for preparing blonanserin

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Abstract

The invention relates to a method for preparing a compound blonanserin in a formula (I), which comprises a step of transforming a compound in a formula (II) and N-ethylpiperazine under the catalysis of base into the compound blonanserin in the formula (I). The blonanserin has extremely valuable pharmacodynamic and treatment properties in the aspect of treating schizophrenia.

Description

technical field The present invention relates to synthetic formula (I) compound blonanserin, i.e. 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9, Process for the preparation of 10-hexahydrocyclooctane[b]pyridine. Background technique Blonanserin has a strong blocking effect on dopamine D2 receptors and 5-tryptamine receptors, and is a new generation of anti-schizophrenic drugs with valuable pharmacological properties. Therefore, the development of PN will bring better economic and social benefits. Regarding the preparation of blonanserin, a method for preparing blonanserin by high-temperature reaction has been described in EP 0385237, and its route is as follows: This route takes 2-chloro-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocyclooctane [b] pyridine and N-ethylpiperazine as raw materials, in the absence of Catalyst and solvent-free high-temperature melting reaction to prepare blonanserin with a yield of 47%. The disadvantage of the above method is that ...

Claims

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Application Information

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IPC IPC(8): C07D221/04A61K31/496A61P25/18B01J27/236B01J27/232
Inventor 张志强卢文李萍
Owner BEIJING D VENTUREPHARM TECH DEV
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