A kind of preparation method of dezocine impurity a and its homologue

A homologue, dezocine technology, applied in the direction of organic chemistry, etc., to achieve the effect of simple and easy to obtain reagents and convenient operation
CN109206385BActive Publication Date: 2022-04-22YANGTZE RIVER PHARM GRP CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
YANGTZE RIVER PHARM GRP CO LTD
Publication Date
2022-04-22

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Abstract

The invention discloses a preparation method of dezocine impurity A and its homologues, which comprises the following steps: using dezocine and its homologues as raw materials, using transition metals as catalysts, and peroxides as oxidants, reacting to obtain dezocine Octane impurity A and its homologues. The invention has the advantages of providing a new chemical method for converting phenolic substances into epoxides, meanwhile, the reagents used are simple and easy to obtain, the operation is simple, and some unreacted raw materials can be recovered.
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Description

technical field

[0001] The invention belongs to the field of medicinal chemistry, and in particular relates to a preparation method of dezocine impurity A and its homologues. Background technique

[0002] Dezocine is a typical opioid alkaloid analgesic, developed by AstraZeneca, and belongs to a synthetic mixed opioid receptor agonist-antagonist. Due to the good tolerance and safety of dezocine, the recognition of the market and medical institutions has been continuously improved, and the clinical demand has continued to increase. Dezocine is less addictive and is used to treat moderate to severe postoperative pain, visceral colic, and pain in patients with advanced cancer. At present, dezocine has been approved for marketing by the State Food and Drug Administration of China, and its synthesis process has been industrialized (CN102503840A). Dezocine is prone to degradation reaction during the stability test, resulting in impurity A, whose chemical structure is as follows:...

Claims

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