A kind of preparation method of cariprazine

A cariprazine and system technology, applied in the direction of organic chemistry, etc., can solve the problems of unstable temperature, process impurities, only 75-80%, etc., and achieve the advantages of less route steps, simple process, and improved yield and reaction speed. Effect
CN110317182BActive Publication Date: 2021-10-15SHANGYU JINGXIN PHARMA +2

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
SHANGYU JINGXIN PHARMA
Publication Date
2021-10-15

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Abstract

The invention provides a kind of preparation method of cariprazine, it comprises the steps: trans-2-(trans-4-(3,3-dimethylureido) cyclohexyl) derivative reacts in acid-binding agent Reaction with 1‑(2,3‑dichlorophenyl)piperazine or its salts under conditions, followed by reaction with reducing agent to generate cariprazine. The synthesis route of cariprazine of the present invention has few steps, simple process and meets production requirements.
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Description

technical field

[0001] The invention relates to medicinal chemistry, in particular to a preparation method of cariprazine. Background technique

[0002] The structural formula of Cariprazine is shown as the compound of formula A. It was jointly developed by Gedeon Richter Ltd and Forest Laboratories. It was first reported that it has a dopamine D3 / D2 partial agonist, and it has both preferential binding to D3R and DA partial agonists. It is used for the treatment of schizophrenia, mania, and severe depression. Its hydrochloride was listed in the United States as an anti-schizophrenia drug in 2015. The chemical name is trans-1-{4-[2-[ 4-(2,3-Dichlorophenyl)-piperazin-1-yl]ethyl]cyclohexyl}-3,3-dimethylurea hydrochloride.

[0003]

[0004] There are documents to disclose the cariprazine synthesis process route as follows:

[0005]

[0006] As can be seen from the above synthetic route, in the process of synthesizing cariprazine, the classic synthesis process has the fo...

Claims

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