Method for synthesizing 6-chlorhydroxyl indole

A technology of looxindole and its synthesis method, which is applied in the direction of organic chemistry, can solve the problems of no patent publications and process characteristics that cannot meet industrial production, so as to improve safety and operation controllability, and reduce post-processing procedures , mild effect
CN104744338AInactive Publication Date: 2015-07-01天津维智精细化工有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
天津维智精细化工有限公司
Publication Date
2015-07-01
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to a method for synthesizing 6-chlorhydroxyl indole. The synthesizing steps are as follows: (1) preparing 2, 5-dichloronitrobenzene through paradichlorobenzene nitration; (2) synthesizing 2-(4-chlorine-2-nitrobenzophenone) dimethyl malonate by 2, 5-dichloronitrobenzene; (3) synthesizing 4-chlorine-2-nitrophenyl acetic acid by 2, 5-dichloronitrobenzene; and (4) preparing 6-chlorhydroxyl indole by 4-chlorine-2-nitrophenyl acetic acid. By adopting the method, the whole reaction process is mild in condition and easy to control; the safety in the reaction process is increased, the operation is simple and the industrial production can be realized; and the raw materials are simple and easy to obtain, the production cost is reduced, the yield is obviously increased and a foundation for the industrial production is laid.
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Description

technical field

[0001] The invention relates to a preparation method of a drug intermediate, in particular to a method for synthesizing the intermediate 6-chlorooxindole of the drug ziprasidone hydrochloride. Background technique

[0002] Ziprasidone hydrochloride (Ziprasidone) is the latest atypical broad-spectrum antipsychotic drug developed for the treatment of schizophrenia. This product is a 5-hydroxytryptamine and dopamine receptor antagonist, especially for 5-HTA2 / DAD2 receptors with strong affinity. The oral dosage form and intramuscular injection dosage form of the drug were launched in Sweden in September 1998 and 2000, respectively. It has a good curative effect on acute or chronic, initial or recurrent schizophrenia; it is effective on schizophrenia-related symptoms (including audiovisual hallucinations, delusions, lack of motivation and social evasion). Compared with traditional antipsychotic drugs, the drug can not only improve positive symptoms, but also neg...

Claims

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