Method for preparing trenbolone acetate

A technology of trenbolone acetate and acid solution, which is applied in the field of preparation and processing of hormone drugs, can solve the problems of no obvious improvement in total yield, difficulty in purification, serious environmental pollution, etc., and achieves high production cost and operability, high raw material Inexpensive and easy to obtain, the effect of simple reaction control

Inactive Publication Date: 2019-11-12
ZHEJIANG SHENZHOU PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
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Problems solved by technology

[0009] This route first carries out the esterification of the 17-hydroxyl group, which limits the possibility of trenbolone being esterified by other esters. It is difficult to control the selective hydrolysis of enol esters, and it is prone to incomplete or excessive hydrolysis, resulting in difficulties in purification and large-scale production.
[0010] The route disclosed in Chinese patent CN102924553 (Common Pharmaceutical Industry) is to change the acidic catalyst in the route reported by Zhang Huyue and others from p-toluenesulfonic acid to acetyl chloride/methanol. This

Method used

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  • Method for preparing trenbolone acetate
  • Method for preparing trenbolone acetate
  • Method for preparing trenbolone acetate

Examples

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example 1

[0039] Example 1 reduction reaction: 3-ethylenedioxyestradiol-Δ 5,10 ,Δ 9,11 - Preparation of Dien-17-ols 1

[0040] Add 10 grams of 3-ethylenedioxyeststrone-Δ to the reaction flask 5,10 ,Δ 9,11 - Diene-17-one (1), 80 ml of isopropanol, 5 g of sodium borohydride, heated to 60 ° C and stirred for reaction, after the reaction was completed, cooled to 10 ° C, water analysis, filtered to precipitate solids, and dried to obtain 9.2 g of 3-ethylenedioxyestr-Δ 5,10 ,Δ 9,11 - Dien-17-ol (2).

example 2

[0041] Example 2 reduction reaction: 3-ethylenedioxyestradiol-Δ 5,10 ,Δ 9,11 - Preparation of Dien-17-ol 2

[0042] Add 10 grams of 3-ethylenedioxyeststrone-Δ to the reaction flask 5,10 ,Δ 9,11- Diene-17-one (1), 100 ml of ethanol, 10 g of potassium borohydride, controlled temperature 0 ° C, stirred and reacted, after the reaction was completed, cooled to -5 ° C, water analysis, filtered to precipitate solids, dried to obtain 9.1 gram 3-ethylenedioxyestr-Δ 5,10 ,Δ 9,11 - Dien-17-ol (2).

example 3

[0043] Example 3 reduction reaction: 3-ethylenedioxyestradiol-Δ 5,10 ,Δ 9,11 - Preparation of Dien-17-ol 3

[0044] Add 10 grams of 3-ethylenedioxyeststrone-Δ to the reaction flask 5,10 ,Δ 9,11 - Dien-17-one (1), 80 ml of methanol, 5 g of potassium borohydride, heated to 40 ° C and stirred for reaction, after the reaction was completed, cooled to 6 ° C, water analysis, filtered to precipitate solid, and dried to obtain 9.0 g 3-ethylenedioxyestr-Δ 5,10 ,Δ 9,11 - Dien-17-ol (2).

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Abstract

The invention discloses a method for preparing trenbolone acetate, and belongs to the technical fields of preparation and processing of hormone drugs. According to the method, 3-ethylenedioxy-estra-[delta]<5,10>,[delta]<9,11>-dien-17-one is used as an initial raw material, keto at a 17th position is reduced into an alcohol, a ketal group at a 3rd position is hydrolyzed, oxidative dehydrogenation is performed, and acetylation is performed on an alcohol group at a 17th position to prepare the trenbolone acetate. The synthetic process route of the trenbolone acetate provided by the invention hasthe advantages of cheap and easily available raw materials, simple and convenient reaction control, few byproducts, easy purification, a high total yield and extremely-high competitiveness in production cost and operability, is suitable for industrial large-scale production, and has good economic benefits.

Description

technical field [0001] The invention relates to the technical field of preparation and processing of hormone drugs, in particular to a method for preparing trenbolone acetate. Background technique [0002] Trenbolone Acetate (Trenbolone Acetate), the chemical name is 17β-acetoxy-estra-4,9,11-trien-3-one, is a kind of anabolic hormone with good effect, which can significantly promote the At the same time, it can significantly reduce the ratio of meat to feed and improve meat quality. As a growth agent for beef cattle, it has been mass-produced and widely used abroad, especially in North America. Due to its preventive effect against mad cow disease, the demand for trenbolone acetate is increasing. [0003] The synthetic route of existing trenbolone acetate is relatively long, and some reaction yields are extremely low, which makes it very difficult to obtain the crystallization of the final product. (Fudan Journal (Medical Edition) 2002, 29 (3): 211-212) reported a preparati...

Claims

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Application Information

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IPC IPC(8): C07J1/00
CPCC07J1/0074
Inventor 王友富邵振平王荣王炳乾
Owner ZHEJIANG SHENZHOU PHARMA
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