Synthesis method of dutasteride intermediate

A synthetic method, dutasteride technology, applied in the direction of steroids, organic chemistry, etc., can solve the problems of high price, high cost, unsuitable for large-scale industrial production, etc., to achieve increased yield, improved safety, reduced cost effect
CN102746368AInactive Publication Date: 2012-10-24王履诚
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
王履诚
Publication Date
2012-10-24
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to a synthesis method of a dutasteride intermediate, belonging to the field of medicament. The synthesis method comprises the steps of dissolving 3-oxo-4-aza-androst-5-ene-17beta-carboxamide in organic solvent, adjusting pH value, stirring at room temperature, slowly adding reducing agent NaBH3CN, carrying out hydrogenation reaction for 1h, adjusting pH value with 10% NaOH solution, extracting with CH2Cl2, drying, filtering, evaporating filtrate under reduced-pressure to be dry to obtain crude product and recrystallizing the crude product. The synthesis method has the advantages that the ratio of the obtained alpha-isomer is high, the yield is higher, the production cost is simultaneously reduced, and the experiment safety is improved.
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Description

technical field

[0001] The invention belongs to the field of medicine and relates to the synthesis of pharmaceutical intermediates, in particular to a synthesis method of a dutasteride intermediate, namely 3-oxo-4-aza-5α-androster-17β-carboxamide. Background technique

[0002] Benign prostatic hyperplasia (benign prostate hyperplasia, BPH) is a common chronic disease in middle-aged and elderly men. The main clinical drugs for the treatment of BPH are finasteride and dutasteride. Dutasteride (Avodart) belongs to azasteroid compounds, and is a selective inhibitor of type I and type II 5α reductase. Its curative effect is better than that of finasteride, and its side effects are low. It is a new type of treatment for benign prostate Drugs for proliferation.

[0003] Dutasteride, chemical name: (5α, 17β)-N-[2,5-bis(trifluoromethyl)phenyl]-3-oxo-4-aza-androstine-1-ene- 17-carboxamide, the structural formula is (Ⅲ); 3-oxo-4-aza-5α-androst-17β-carboxamide is a key intermediate f...

Claims

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