Method for preparing boldenone through selective reduction

A Boldenone and selectivity technology, which is applied in the field of preparation of pharmaceutical compounds, can solve the problems of prolonging the production cycle, increasing production costs, increasing reaction steps, etc., and achieve the effects of reducing production processes, low cost, and improving selectivity

Inactive Publication Date: 2015-02-04
HUAZHONG PHARMA
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The existing preparation process of Boldenone increases the reacti...

Method used

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  • Method for preparing boldenone through selective reduction
  • Method for preparing boldenone through selective reduction
  • Method for preparing boldenone through selective reduction

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Add 350ml of methanol and 100ml of water into the reaction flask, stir and cool down to -10°C, and add 4.5g of sodium borohydride. Then add 50 g of 1,4-androstenedione that has been crushed and passed through a 20-mesh sieve in portions at -10°C to -5°C, and the time for adding 1,4-androstenedione is 20 minutes to 30 minutes. After the addition is complete, continue to stir and react at -10°C to -5°C for 0.5 hours. The reaction solution was added to water cooled to 0°C-5°C in advance, stirred at 0°C-5°C for 0.5 hour, filtered with suction and dried to obtain 49.7 g of crude product. The crude product was then crystallized from a mixed solvent of methanol and ethyl acetate to obtain 47.6 g of Boldenone with an HPLC purity of 98.6%.

Embodiment 2

[0034] Add 350ml of methanol and 50ml of water into the reaction flask, stir and cool down to -10°C, and add 5.5g of potassium borohydride. Then add 50 g of 1,4-androstenedione that has been crushed and passed through a 20-mesh sieve in portions at -10°C to -5°C, and the time for adding 1,4-androstenedione is 20 minutes to 30 minutes. After the addition is complete, continue to stir and react at -10°C to -5°C for 45 minutes. The reaction solution was added to water cooled to 0°C-5°C in advance, stirred at 0°C-5°C for 0.5 hour, filtered with suction and dried to obtain 49.5 g of crude product. The crude product was crystallized from a mixed solvent of methanol and ethyl acetate to obtain 47.5 g of Boldenone, with an HPLC purity of 98.6%.

Embodiment 3

[0036]Add 350ml of methanol and 60ml of water into the reaction flask, stir and cool down to -10°C, and add 5g of potassium borohydride. Then add 50 g of 1,4-androstenedione that has been crushed and passed through a 20-mesh sieve in portions at -10°C to -5°C, and the time for adding 1,4-androstenedione is 20 minutes to 30 minutes. After the addition is complete, continue to stir and react at -10°C to -5°C for 45 minutes. The reaction solution was added to water cooled to 0°C-5°C in advance, stirred at 0°C-5°C for 0.5 hour, filtered with suction and dried to obtain 49.6 g of crude product. The crude product was then crystallized from a mixed solvent of methanol and ethyl acetate to obtain 47.6 g of boldenone, with an HPLC purity of 98.5%.

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Abstract

The invention provides a method for preparing boldenone through selective reduction. 1,4-androstenedione is used as a main raw material, the charging sequence is changed, the main raw materials are treated in advance, the charging mode of the main raw materials is changed, and the keto selective reduction reaction is carried out, thus, the boldenone is prepared. The method solves the problems that the existing boldenone preparation process has more steps, long period and high production cost. According to the preparation method, the production procedures are reduced, the production period is shortened, the operation is simple, the cost is low and the method is suitable for industrial production.

Description

technical field [0001] The present invention relates to a method for preparing pharmaceutical compounds, in particular to a method for selectively reducing boldenone (17β-hydroxyl-1,4-androstadien-3-one). Background technique [0002] The structural formula of Boldenone (17β-hydroxy-1,4-androstadien-3-one, CAS: 846-48-0) is: [0003] [0004] Boldenone (Boldenone) is a derivative of testosterone, which has clinical effects such as strongly enhancing blood vessel supply, strengthening muscles, highlighting blood vessels, and increasing appetite. [0005] There are many manufacturers of 4-androstenedione (4AD) and 1,4-androstenedione (ADD) produced by sterol bio-fermentation in China, and the supply of raw materials is very sufficient. 4AD and ADD, which are cheap and easy to buy, are widely used as key intermediates of steroid hormone drugs. The existing technology of Boldenone is exactly to prepare with aforementioned two kinds of raw materials respectively, specificall...

Claims

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Application Information

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IPC IPC(8): C07J1/00
CPCC07J1/0022
Inventor 廖俊曾建华冯旋魏旭力付林
Owner HUAZHONG PHARMA
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