Novel method for removing methyl impurity in preparation of asenapine

A technology of asenapine maleate and demethylation, which is applied in the field of new process synthesis to achieve the effect of simple process, high quality and easy access to raw materials

CN105566336AInactive Publication Date: 2016-05-11AVENTIS PHARMA HAINAN
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
Publication Date
2016-05-11
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to a novel method for removing the methyl impurity in the preparation of asenapine. According to the method, asenapine maleate is taken as the raw material, then asenapine maleate is decomposed, the free alkalis and ethyl chloroformate are refluxed in toluene, and the product reacts with hydrobromic acid under reflux to obtain the methyl-free asenapine product. The method has the advantages of high yield and simple and convenient operation.
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