Method utilizing cyclodextrin to assist plant sterol composition to prepare androstane-4-ene-3,17-diketone

Abstract

The invention relates to a method utilizing cyclodextrin to assist a plant sterol composition to prepare androstane-4-ene-3,17-diketone, and provides a preparation method utilizing nocardia or mycobacterium to ferment a plant sterol composition so as to obtain androstane-4-ene-3,17-diketone and / or androstane-1,4-diene-3,17-diketone, wherein cyclodextrin is added during the fermentation process, and the mole ratio of the cyclodextrin to the plant sterol composition is 1:10 to 1:2.

Description

field of invention [0001] The present invention generally relates to a process for the preparation of androst-4-ene-3,17-dione, which effectively improves the production of androst-4-ene with a phytosterol composition as a substrate by adding a small amount of cyclodextrin The yield of -3,17-diketone shortens the fermentation time, which is very beneficial to industrialization. Background technique: [0002] Androst-4-ene-3, 17-dione (androst-4-ene-3, 17-dione, referred to as androstenedione or AD) is an irreplaceable intermediate of steroid hormone drugs, which plays an important role in the body. very important regulation. It can be said that almost all steroid hormone drugs are produced with AD as the starting material. Such as for the production of sex hormones, progesterone, anabolic hormones and corticosteroids, but also for the synthesis of more than 100 kinds of drugs such as hydrocortisone, prednisone oxide, progesterone, estrenol, dexamethasone, etc. It is an es...

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Problems solved by technology

Yang Ying pointed out in the article (Research progress of microbial degradation of sterol side chain and conversion of androst-4-ene-3??17-dione, Microbiology Bulletin, 2006 33 (6), 142-145) sterol substrates in The problem of poor solubility and serious product (substrate) inhibition in aqueous media has plagued the entire steroid industry. Sterols are hydrophobic compounds with extremely low solubility in water, which leads to incompatible substrates and microbial cells. Good contact, lower conversion rate and longer conversion time

[0006] Utilize mycobacterium to carry out fermentation at the same time, the time is longer, often up to 72 hours, many papers all have been introduced to this, for example CN03804973, and the problem of long-time fermentation is that at first it is easy to cause excessive fermentation of microorganisms, the obtained AD / ADD is converted into 9α-hydroxytestosterone and even the steroid ring is degraded. Secondly, the reaction time is too long, which will increase the number of miscellaneous bacteria, and the conversion specificity of the culture bacteria will decrease, thereby increasing impurities. Thirdly, the long-term reaction will also cause production cycles. , manufacturing costs, labor costs, etc. are rising, which is not conducive to industrialization

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