A kind of method of synthesizing cariprazine

A technology of piperazine and dichlorophenyl, applied in the field of synthesizing cariprazine, can solve the problems of long total reaction steps, expensive reagents and equipment requirements, etc., and achieve the effect of increasing the total yield and shortening the process steps
CN108586389BActive Publication Date: 2020-06-12成都福柯斯医药技术有限公司
17 Cites 0 Cited by

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
成都福柯斯医药技术有限公司
Publication Date
2020-06-12

Smart Images

  • Figure 1
    Figure 1
  • Figure 2
    Figure 2
  • Figure 3
    Figure 3
Patent Text Reader

Abstract

The invention belongs to the technical field of organic synthesis, and provides a novel method for synthesizing cariprazine. The novel method comprises the following steps: firstly, carrying out condensation reaction on trans-2-(4-(3,3-dimethyl ureido) cyclohexyl) acetic acid and 1-(2,3-dichlorophenyl) piperazine to obtain 3-(trans-4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-2-oxo-ethyl}-cyclohexyl)-1,1-dimethylurea; and secondly, reducing 3-(trans-4-{2-[4-(2,3-dichlorophenyl)-piperazine-1-yl]-2-oxo-ethyl}-cyclohexyl)-1,1-dimethylurea by using borane to obtain the cariprazine. The method hasthe advantages that process steps are greatly shortened, the purity of a final product is ensured and the total yield is obviously increased.
Need to check novelty before this filing date? Find Prior Art

Description

technical field

[0001] The invention belongs to the field of organic synthesis, and in particular relates to a method for synthesizing cariprazine. Background technique

[0002] Cariprazine (Cariprazine, CAS registration number: 839712-12-8), is a third-generation antipsychotic new drug jointly developed by Allergan of the United States and Gedeon Richter Pharmaceutical Company of Hungary, for the treatment of schizophrenia, mania, and severe depression syndrome; on September 17, 2015, it was approved for marketing by the US Food and Drug Administration. Its chemical name is trans-4-{2-[4-(2,3-dichlorophenyl)-piperazin-1-yl]-ethyl}-N,N-dimethylformyl-cyclohexyl Amine, the structural formula is as follows:

[0003]

[0004] 国际专利WO2015056164、WO20111060363、WO2010070370、WO2010070371、WO2008142461和WO2005012266以及文献JMC2013,56(22),9199-9221,Bioorganic&Medicinal Chemistry Letters,22,(2012),3437-3440均报道了卡利拉嗪的合成方法, Summarized as follows:

[0005]

[0006] Among them, Compound ...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More