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Method for synthesizing Piberacine precursor

A synthetic method and compound technology, applied in the field of synthesis of piperacine precursors, can solve problems such as unestablished, and achieve the effects of safe use, saving labor, electricity and freight, and high yield

Inactive Publication Date: 2009-09-30
HEILONGJIANG HUAXIN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Therefore, the method of industrial production of MC has not been established so far

Method used

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  • Method for synthesizing Piberacine precursor
  • Method for synthesizing Piberacine precursor
  • Method for synthesizing Piberacine precursor

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Embodiment Construction

[0028] The purpose of the present invention is to provide a method beneficial to industrial production of MC.

[0029] 1. Preparation process

[0030] by and (X represents Cl or Br atom)

[0031] After the reaction, react with triphenylphosphine to obtain the following formula

[0032]

[0033] Reaction with 3.4.5-benzoic acid benzaldehyde to obtain the following formula

[0034]

[0035] Maleic acid reacts with the piperacine precursor represented by formula ④ to generate

[0036]

[0037] According to the present invention, at first by the reaction of formula ⑦ and the compound represented by formula ⑧, then react with three phosphine.

[0038] The reaction of formula ⑦ and formula ⑧ can be carried out in the following solvents: chloroform, benzene, xylene, ether, cyclohexane and other solvents. The ratio of the reactants of formula ⑦ and formula ⑧ is not particularly limited, and can be selected within a wide range. Generally, the ratio of the former to th...

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PUM

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Abstract

The raw material of the invention is cheap and easy to obtain, usage is safe. It is not only capable of setting a lower and milder reaction temperature, also the reaction resultant of each step reaction need not to separate, and the process may be carried continuously until a final product is obtained. It is capable of completing by one step, and completing by two steps even though a treating process is included. The operational process of the invention is simple, and it is capable saving burden charges such as manpower, electric force, carriage freight and the like. The reactant of each step need not to separate accurately, thus the loss is less and the yield is high. The synthesizing method is very convenient without usage of thionyl chloride. Reaction is favorable, and it is easy of the industrial production.

Description

[technical field] [0001] The present invention relates to the synthesis method of pibelacine precursor. The piperacine precursor synthesized by the present invention is represented by the following formula ①. [0002] [0003] Piperacine maleate represented by the above formula is an important compound as a cerebral circulation metabolism improving agent. (Hereafter expressed as MC). [Background technique] [0004] As the synthetic method of MC, for example: the method described in No. 45-9740 of patent announcement, 47-1293, 47-27233, 49-20191, 49-20192, 51-101988, No. 730345 etc., above these methods are basically the same, with The method recorded in Announcement No. 47-1293 is representative, and will be described in detail. [0005] The method described in the announcement is shown in the following reaction: formula ② reacts with formula ③ to generate the precursor of pipelacine of formula ④, and then reacts with maleic acid to obtain the target product MC. [00...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D295/185C07F9/6558
Inventor 张立国
Owner HEILONGJIANG HUAXIN PHARMA
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