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Preparation method of 6-dehydronandrolone acetate

A technology of nandrolone acetate and diacetate, applied in the directions of steroids, organic chemistry, etc., can solve the problems of many synthesis steps of steroids, difficult separation and purification, complicated reactions, etc., and achieves environmental friendliness and simple operation process. , mild conditions

Inactive Publication Date: 2017-11-17
YICHENG GOTO PHARMA
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Problems solved by technology

[0002] Steroidal drugs play an important role in the prevention and treatment of diseases, including medicine, veterinary drugs and pesticides. There are more than 400 kinds of steroidal drugs that have been marketed in foreign countries, and the existing varieties in my country account for only one-third of them, which is far from the world's advanced level. There is still a certain gap in the research and development of steroid drugs compared with the advanced countries in the world. The main performance is that there are many steps in the synthesis of steroid drugs, the reaction is complicated, the long-range effect of the group is very obvious, and the yield is low. Difficulty in separation and purification

Method used

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  • Preparation method of 6-dehydronandrolone acetate
  • Preparation method of 6-dehydronandrolone acetate
  • Preparation method of 6-dehydronandrolone acetate

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Embodiment Construction

[0021] General reaction formula of the present invention is

[0022]

[0023] The present invention puts a No. 8 magnet in a 100mL three-necked flask, and dissolves the compound 3,5-estradiene-3,17β-diacetate (1g) in DMF (3.78g) and water (62mg) In the mixed solution, maintain the reaction temperature of the system at -10°C to -5°C. At this temperature, a solution of NBS (0.535 g) dissolved in DMF (1.65 g) was added dropwise while maintaining the reaction temperature below 0°C. After the feeding was completed, the mixture was heated to 25° C. within 30 min, and the reaction was detected by TLC. After the reaction is completed, first add sodium carbonate (0.495g) to the system, and then add sodium bromide (0.255g) to the system after the reaction is complete. React for half an hour, and then within one hour, gradually raise the temperature to 80°C, and continue the reaction for 3 hours until the end of the reaction. Stop heating after the reaction is over, cool the reacti...

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Abstract

Steroid drug tibolone is a drug for treatment of functional disorder diseases in climacteric or postoperative menopausal women. According to the route, estra-3, 5-diene-3, 17beta-diacetate is adopted as the raw material to undergo bromine addition so as to complete alkene displacement and synthesize 6-dehydronandrolone acetate. The drug is one of the important pro-drugs of tibolone, and the yield is 85%. The 6-dehydronandrolone acetate steroid drug synthesis method provided by the invention has the advantages of simple and easy operation, and high yield.

Description

technical field [0001] The invention belongs to the field of medicine synthesis, and in particular relates to a preparation method of 6-dehydronandrolone acetate steroid medicine. Background technique [0002] Steroidal drugs play an important role in the prevention and treatment of diseases, including medicine, veterinary drugs and pesticides. There are more than 400 kinds of steroidal drugs that have been marketed in foreign countries, and the existing varieties in my country account for only one-third of them, which is far from the world's advanced level. There is still a certain gap in the research and development of steroid drugs compared with the advanced countries in the world. The main performance is that there are many steps in the synthesis of steroid drugs, the reaction is complicated, the long-range effect of the group is very obvious, and the yield is low. Separation and purification are difficult. The research on many steroidal drugs, especially the steroidal dr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J1/00
CPCC07J1/0074
Inventor 李栋张谦潘高峰卢方欣系祖斌贺一君
Owner YICHENG GOTO PHARMA
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