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Preparation process of cyproterone acetate

A technology for the preparation of cyproterone acetate, which is applied in the chemical industry, can solve the problems of not being well adapted to industrial production, benzene residues, and low total yields, and achieves overcoming the problems of benzene residues, stable reactions, and high total yields. high effect

Inactive Publication Date: 2018-08-17
YUEYANG HUANYU PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Cyproterone acetate, also known as cyproterone acetate, cyproterone ester, cyproterone, cyproterone acetate, is a male hormone antagonist, has a strong anti-androgen effect, and also has progesterone Active, it can be used clinically to treat abnormal libido, prostatic hypertrophy and prostate cancer, precocious puberty, women's hirsutism, acne, menopausal syndrome and sequential application of hormone replacement therapy with estradiol valerate, etc. In the process, benzene with high toxicity is usually used, and there are difficult benzene residue problems in the process products, and the total yield is low, so it cannot be well adapted to industrial production

Method used

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  • Preparation process of cyproterone acetate
  • Preparation process of cyproterone acetate
  • Preparation process of cyproterone acetate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Ketal reaction: pump dichloromethane, ethylene glycol, and triethyl orthoformate into the reaction kettle, add dehydrogenation substance, PTS, and react at a temperature of 30°C for 5 hours, add triethylamine to neutralize the pH to 8, negative Concentrate under pressure to recover dichloromethane, add methanol, freeze and crystallize until thick, centrifuge, and dry to obtain the ketal product;

[0019] Cyclopropane hydrolysis reaction: Add DMF, ketal and TBS salt in the reaction kettle, add caustic soda three times under stirring at 42°C, react for 3 hours after addition, add the prepared dilute sulfuric acid to adjust the pH value to 2 and hydrolyze for 2 hours After the hydrolysis, the material is pumped to the water analysis tank for water analysis, centrifuged, washed with water until neutral, and dried to obtain cyclopropane hydrolyzate;

[0020] Acetyl reaction: pump chloroform and acetic anhydride into the reactor, add cyclopropane hydrolyzate and PTS, heat up ...

Embodiment 2

[0026] Ketal reaction: pump dichloromethane, ethylene glycol, and triethyl orthoformate into the reaction kettle, add dehydrogenate, PTS, react at a temperature of 31°C for 5 hours, add triethylamine to neutralize the pH to 8, negative Concentrate under pressure to recover dichloromethane, add methanol, freeze and crystallize until thick, centrifuge, and dry to obtain the ketal product;

[0027] Cyclopropane hydrolysis reaction: Add DMF, ketal and TBS salt in the reaction kettle, add caustic soda three times under stirring at 43°C, react for 3 hours after addition, add the prepared dilute sulfuric acid to adjust the pH value to 2 and hydrolyze for 2 hours After the hydrolysis, the material is pumped to the water analysis tank for water analysis, centrifuged, washed with water until neutral, and dried to obtain cyclopropane hydrolyzate;

[0028] Acetyl reaction: pump chloroform and acetic anhydride into the reaction kettle, add cyclopropane hydrolyzate and PTS, heat up to 59°C ...

Embodiment 3

[0034] Ketal reaction: pump dichloromethane, ethylene glycol, and triethyl orthoformate into the reaction kettle, add dehydrogenate, PTS, and react at a temperature of 32°C for 5 hours, add triethylamine to neutralize the pH to 8, negative Concentrate under pressure to recover dichloromethane, add methanol, freeze and crystallize until thick, centrifuge, and dry to obtain the ketal product;

[0035] Cyclopropane hydrolysis reaction: Add DMF, ketal and TBS salt into the reaction kettle, add caustic soda three times under stirring at 45°C, add reaction for 3 hours, add the prepared dilute sulfuric acid to adjust the pH value to 2 and hydrolyze for 2 hours After the hydrolysis, the material is pumped to the water analysis tank for water analysis, centrifuged, washed with water until neutral, and dried to obtain cyclopropane hydrolyzate;

[0036] Acetyl reaction: pump chloroform and acetic anhydride into the reaction kettle, add cyclopropane hydrolyzate and PTS, heat up to 60°C an...

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Abstract

The invention relates to a preparation process of cyproterone acetate. The preparation process of cyproterone acetate specifically comprises the following steps of ketalation reaction, cypro-hydrolysis reaction, acetyl reaction, epoxy reaction, chlorination reaction and cyclization reaction. The preparation process of cyproterone acetate can overcome the problem of benzene residues difficult to solve in original process products and is simple in initial raw materials, stable in reaction and high in total yield.

Description

technical field [0001] The invention relates to the technical field of chemical industry, in particular to a preparation process of cyproterone acetate. Background technique [0002] Cyproterone acetate, also known as cyproterone acetate, cyproterone ester, cyproterone, cyproterone acetate, is a male hormone antagonist, has a strong anti-androgen effect, and also has progesterone Active, it can be used clinically to treat abnormal libido, prostatic hypertrophy and prostate cancer, precocious puberty, women's hirsutism, acne, menopausal syndrome and sequential application of hormone replacement therapy with estradiol valerate, etc. In the process, benzene with high toxicity is usually used, and there are difficult benzene residue problems in the process products, and the total yield is low, which cannot be well adapted to industrial production. Contents of the invention [0003] In order to solve the problems proposed in the above-mentioned background technology, the objec...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J53/00
CPCC07J53/004
Inventor 徐润星
Owner YUEYANG HUANYU PHARMA
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