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

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...

AI Technical Summary

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, providing a microbial fermentation dehydrogenation method to increase the yield of 17а-hydroxypregna-1,4,6-triene-3,20-dione products, and reduce environmental pollution to prepare color dragon way