A kind of preparation method and refining method of olanzapine

A refining method, the technology of olanzapine, applied in the direction of organic chemistry, etc., can solve the problems of increasing the difficulty of quality control, limited source of raw materials, increasing production costs, etc., and achieve the effect of high yield, simple process and low pollution
CN102268010AInactive Publication Date: 2011-12-07大连美罗大药厂 +3
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
大连美罗大药厂
Publication Date
2011-12-07
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to a preparation method and a refining method of olanzapine, belonging to the field of medicine preparation. 4-amino-2-methyl-10H-thieno[2,3-b][1,5]-benzodiazepine hydrochloride and N-methylpiperazine reflux reaction, or in diethylene di Refluxing reaction in alcohol dimethyl ether, after the reaction is over, vacuum distillation recovers excess N-methylpiperazine or vacuum distillation recovers excess N-methylpiperazine and diethylene glycol dimethyl ether solvent to obtain olanzapine solid The crude product is recrystallized with ethanol aqueous solution, filtered and dried to obtain the olanzapine product; then dissolved with ethanol under reflux, decolorized with a decolorizing agent, filtered, and the filtrate is cooled to room temperature for crystallization, filtered and dried to obtain refined olanzapine. The invention has the advantages of avoiding highly toxic solvents in the preparation process, little pollution and safe operation; fast reaction, reducing energy consumption; recovering excessive raw materials and solvents, appropriately reducing costs; high yield; olanzapine The refined product has high purity (>99.5%, HPLC) and stable quality.
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Description

technical field

[0001] The invention relates to a preparation method and a purification method of olanzapine, and belongs to the field of pharmaceutical preparation. Background technique

[0002] 2-Methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5]-benzodiazepine, hereinafter referred to as "olanzapine" "Ping", a new type of atypical antipsychotics. Olanzapine acts on the central nervous system and is a thiophene benzodiazepine class of serotonin and dopamine receptor dual antagonists. It was developed by Eli Lilly and was first listed in the United States in 1996. The structural formula is as follows (I).

[0003]

[0004] Patent US5229382 studies olanzapine and its preparation method separately, and discloses two methods for preparing olanzapine, including: (a) N-methylpiperazine reacts with the compound of formula (III):

[0005]

[0006] In the formula, Q can be -NH 2 , -OH, -SH, where -NH 2 optimal. This process is characterized in that III is reacted w...

Claims

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