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Synthesis technology of finasteride

A technology of finasteride and synthesis technology, applied in the field of synthesis technology of finasteride, can solve the problems of many side reactions, expensive reagents, many by-products and the like, and achieves the effects of easy operation, reduced production cost and mild conditions

Inactive Publication Date: 2009-09-16
重庆浩康医药化工集团有限公司 +1
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The ammonia / ethylene glycol closed-loop used in this synthesis process requires closed high-temperature reaction; the platinum dioxide high-pressure catalytic hydrogenation method has high requirements for equipment, many by-products, and expensive catalysts; benzene selenite anhydride and triphenyl Phosphine-based reagents are expensive and harmful to the environment; at the same time, due to many side reactions and complicated separation and purification, the cost remains high

Method used

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  • Synthesis technology of finasteride
  • Synthesis technology of finasteride
  • Synthesis technology of finasteride

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Experimental program
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Effect test

Embodiment Construction

[0027] The synthetic route is as follows:

[0028]

[0029] The first step, the preparation of 5-carbonyl-17β-carboxylate methyl ester-A-abortion-3,5-cleavage-androst-3-acid (I)

[0030] 200mL of tert-butanol, 10g (31.6mmol) of methyl 3-carbonyl-4-androstene-17β-carboxylate, add a solution of 10g (94.3mmol) of anhydrous sodium carbonate dissolved in 30mL of water under stirring, and add dropwise under reflux A solution of 40g (22.4mmol) of sodium periodate and 390mg (2.47mmol) of potassium permanganate dissolved in 200mL of water was added, then refluxed for 30min, cooled to room temperature, filtered, most of the tert-butanol was evaporated under reduced pressure, iced Adjust the pH to 2 with 6N hydrochloric acid under bath cooling, extract with ethyl acetate, combine the organic layers, wash with saturated sodium chloride solution, dry over anhydrous sodium sulfate, evaporate the solvent under reduced pressure to obtain a transparent oil, add a small amount of petroleum e...

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Abstract

This invention discloses a synthesis technology of finasteride, it takes 3-oxo-4-androstene-17 beta-carboxylic acid methyle as raw material, and synthesizes finasteride through the following five steps, (a). hydrogen peroxide; (b). cyclization; (c). catalyzed hydrogenation reduction; (d). ester-amide condensation into amide; and (e). oxidizing to form double bond. Compare with the existing technology, this technology has short route, high efficiency, simple operation and low cost.

Description

technical field [0001] The invention relates to a process for chemically synthesizing drugs, in particular to a process for synthesizing finasteride. Background technique [0002] Finasteride, English name: Finasteride, chemical name: N-tert-butyl-3-carbonyl-4-aza-5α-androst-1-ene-17β-amide. Finasteride is a 4-azasteroid that is a specific inhibitor of type II 5a-reductase, an intracellular enzyme involved in the metabolism of testosterone to the stronger dihydrotestosterone. Benign prostatic hyperplasia, or enlarged prostate, depends on the conversion of testosterone to dihydrotestosterone in the prostate. This drug can effectively reduce the blood and dihydrotestosterone in the prostate, reduce the weight of the prostate, increase the urinary flow rate, significantly improve the urinary tract obstruction and complications, and significantly reduce the symptoms of the prostate. It is suitable for the treatment of existing Symptoms of benign prostatic hyperplasia (BPH). A...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J73/00B01J31/02B01J23/44A61P13/08
Inventor 蒋勇丁东升李朝亮刘玥
Owner 重庆浩康医药化工集团有限公司
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