A kind of preparation method of asenapine key intermediate

Abstract

The invention provides a chemical synthesis method, in particular to a preparation method of a key intermediate [formula (III)] compound of asenapine capable of serving as a schizophrenia drug. In an anhydrous system, the intermediate [formula (III)] compound is obtained through dehydration of an intermediate [formula (II)] compound and anhydride under the action of a catalyst. The invention further provides a novel method for preparing asenapine by the intermediate [formula (III)]. The provided method has the advantages of simple operation, high yield, environment-friendliness, lower cost, stable technology and the like.

Description

technical field

[0001] The invention relates to a chemical synthesis method, in particular to a preparation method of a key intermediate of Asenapine which can be used as a schizophrenic drug. Background technique

[0002] Asenapine (Asenapine) is the precursor of preparing asenapine maleate, is a broad-spectrum efficient 5-hydroxytryptamine, norepinephrine and dopamine antagonist, has strong antipsychotic activity, therefore It is necessary to study the drug on a large scale, and the research on the intermediate 3 of the drug is very important.

[0003] The chemical name of asenapine is: trans-5-chloro-2,3,3a,12b-tetrahydro-2-methyl-1H-dibenzo[2,3:6,7]oxazepine [4,5-c]pyrrole, its chemical structural formula is:

[0004]

[0005] There are many patents and documents at home and abroad that have reported the preparation method of asenapine, among which US2006229352, US2010152461, WO2011159903 and other patent documents disclose the following methods to prepare asenapine...

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