Synthesis method of alkyl acid testosterone

A synthesis method and technology of alkyl acid, applied in the field of synthesis of alkyl acid testosterone, can solve the problems of large environmental pollution, many by-products, low yield, etc., and achieve the effects of low price, stable market supply, and reduced production cost
CN111995650AActive Publication Date: 2020-11-27ZHEJIANG SHENZHOU PHARMA
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
ZHEJIANG SHENZHOU PHARMA
Publication Date
2020-11-27

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Abstract

The invention discloses a synthesis method of alkyl acid testosterone, and belongs to the technical field of synthesis and processing of medicines. The method comprises the following steps of: taking4-androstenedione (4AD) as an initial raw material, firstly, carrying out enol ether protection on the keto group at the site 3, and reducing carbonyl at the site 17 into hydroxyl; or taking 4-androstenedione (4AD) as an initial raw material, firstly carrying out enol ether protection on the keto group at the site 3, then reducing carbonyl at the site 17 into hydroxyl, then carrying out hydrolysison the site 3 to obtain testosterone, and carrying out esterification and third-site hydrolysis to obtain the testosterone ester after testosterone third-site ketal protection. According to the method disclosed by the invention, the third site is protected during esterification reaction, the generation of impurities can be reduced, and an esterification reaction solvent is a water-insoluble organic solvent, so that after the reaction is completed, products can be directly extracted in a layered manner, a large amount of water does not need to be added to separate out the products, the amountof wastewater is reduced, the solvent can be recycled, and the process is more suitable for industrial production.
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Description

technical field

[0001] The invention relates to the technical field of synthesis and processing of medicines, in particular to a synthesis method of testosterone alkylate. Background technique

[0002] Testosterone is a male hormone drug, which can promote the development and maturation of male sexual organs and secondary sexual characteristics, and can resist estrogen, and promote protein and bone synthesis. Testosterone is used to treat hypogonadism, to supplement the symptoms of insufficient autogenous secretion or the inability to naturally secrete testosterone, so testosterone can be supplemented regularly to maintain the content of testosterone in the blood.

[0003] At present, most of the methods for synthesizing testosterone derivatives are synthesized by the acid chloride method, such as the synthetic method disclosed in the patent CN105732754A, which uses alcoholic hydroxy steroids as a starting material, uses a water-soluble organic solvent as a solvent, and adds...

Claims

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