The preparation method of tetraene intermediate

A technology for intermediates and tetraenes, applied in the field of preparation of tetraenes intermediates, can solve the problems of many by-products, low yield of target products and the like
CN108165602BActive Publication Date: 2020-12-18HUNAN NORCHEM PHARMACEUTICAL CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
HUNAN NORCHEM PHARMACEUTICAL CO LTD
Publication Date
2020-12-18

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Abstract

The invention relates to a preparation method of tetraene intermediates. According to the preparation method, a first compound is converted by Nocardioides simplex to obtain tetraene intermediates; wherein the first compound is represented by a formula I, tetraene intermediates are represented by a formula II, and R in the formula I and the formula II represents H, a halogen atom, an alkyl group,an alkoxyl group, a hydroxyl group, or a phenyl group. According to the preparation method, the first compound is taken as the substrate, only Nocardioides simplex is used to carry out biological conversion; the substrate is subjected to 1,2-dehydrogenation and 21-acetate hydrolysis at the same time; most of the conversion products is target products, the byproduct ratio is low; after purification, the product is white or white-like crystals; relative to the weight of the substrate, the yield is 80-90%; the target product yield is high; through HPLC analysis, the purify of the product is not less than 95%; and the total content of target products and secondary products is not less than 99%.
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Description

technical field

[0001] The invention relates to the field of preparation of pharmaceutical intermediates, in particular to a preparation method of a tetraene intermediate. Background technique

[0002] Steroids have a variety of biological activities, and their applications are very extensive, some of which are used to treat diseases or develop production, such as hydrocortisone for the treatment of allergic diseases, progesterone for contraceptives, spironolactone for diuretics, synthetic steroids Hormone diosgenin, cardiotonic Digoxin, bufotoxin, etc. are all steroidal compounds. The tetraene intermediates can be further synthesized to obtain a series of drugs such as 3TR, fluocinolone, and triamcinolone acetonide, which are widely used in clinical practice.

[0003] In the synthesis route of tetraene intermediates, the appropriate upstream intermediates are usually selected and carried out by biotransformation methods, but the general biotransformation method converts th...

Claims

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