Method for manufacturing cyproterone acetate intermediate 17a-hydroxy progesterone-1, 4, 6-triene-3, 20-diketone

A technology of hydroxyprogesterone and seprolone, which is applied in the field of biochemistry to achieve the effects of strong toxicity, change of environmental pollution and strong reaction selectivity

Inactive Publication Date: 2013-09-11
YUEYANG HUANYU PHARMA
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Problems solved by technology

[0007] The purpose of the present invention is to solve the problem of 17α-hydroxypregna-4,6-diene-3,20-dione to 17α-hydroxypregna-1,4,6-triene-3, Problems existing in 20-diketones, prov...

Method used

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Embodiment

[0020] See Table 1 for the ratio of the culture medium.

[0021] Table 1 Medium ratio

[0022] Name Specification Proportion Actual volume glucose industry 1.2-1.6% 0.3g corn syrup industry 1.8-2.2% 0.4g Peptone Biochemical reagents 0.4-0.6% 0.1g Potassium dihydrogen phosphate industry 0.4-0.7% 0.12g sodium hydroxide industry Appropriate amount Adjust PH to 6.0-6.5 Bubble enemy Industrial (Silicone) 0.01% 0.002ml water Add water to 100% 19ml

[0023] Add corn steeple, glucose, peptone, potassium dihydrogen phosphate, sodium hydroxide, foam enemy, and water into a 100ml seed bottle according to the process ratio, sterilize at 110-112°C, pressure 0.10-0.12MPa for 20 minutes, after cooling, Insert Arthrobacter (0.1%), 30-33°C, shaker speed 100-110 rpm, culture for 16-22 hours, and transfer to a fermentation bottle.

[0024] In a 1000ml fermentation bottle, prepare 200ml of culture medium by mi...

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Abstract

The invention relates to a method for manufacturing a cyproterone acetate intermediate 17a-hydroxy progesterone-1, 4, 6-triene-3, 20-diketone. The method includes performing microbial fermentation and dehydrogenation on 17a-hydroxy progesterone-4, 6-diene-3, 20-diketone to obtain the 17a-hydroxy progesterone-1, 4, 6-triene-3, 20-diketone. Microbial fermentation and dehydrogenation culture media comprise 1.2-1.6(wt)% of glucose, 1.8-2.6(wt)% of corn steep liquor, 0.4-0.6(wt)% of peptone, 0.4-0.7(wt)% of potassium dihydrogen phosphate, 0.01(wt)% of defoamers and the balance water, and the pH (potential of hydrogen) of a mixture of the glucose, the corn steep liquor, the peptone and the potassium dihydrogen phosphate is regulated by a proper amount of sodium hydroxide and then ranges from 6.0 to 6.5. The method has the advantages that the microbial fermentation and dehydrogenation reaction selectivity is high, a product is free of side effects, the purity of the product is 97%, the content of the maximum impurity component is 1.5%, the yield of the product is greatly increased and reaches 80%, and environmental pollution is obviously reduced as compared with the traditional chemical synthesis process.

Description

technical field [0001] The invention belongs to the field of biochemistry, and relates to a method for preparing 17a-hydroxypregna-1,4,6-triene-3,20-dione, an intermediate of chromapron, in particular to a preparation method of microbial fermentation dehydrogenation Process for the intermediate 17а-hydroxypregna-1,4,6-triene-3,20-dione of chromapron. Background technique [0002] Cyproterone Acetate (chemical name: cyproterone acetate), molecular formula is C 24 h 29 ClO 4 , molecular weight 416.95. The trade name is Cyproterone Acetate, which is an anti-androgen and has the effect of inhibiting male hormones (androgens). It is used for the treatment of abnormal libido in men; inoperable prostate cancer; severe virilization signs in women; it can also be used as a short-acting oral contraceptive. [0003] The existing preparation process of Sepron is to react 17а-hydroxyprogesterone (I) to obtain 6,7-dehydrogenate (II) (17а-hydroxypregna-4,6-diene-3,20-dione ), 6,7-deh...

Claims

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Application Information

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IPC IPC(8): C12P33/02C12R1/06
Inventor 朱福忠周伟文李慧李杰
Owner YUEYANG HUANYU PHARMA
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