Method for preparing steroid anti-inflammatory medicine prednisolone acetate by adopting enzyme process

A technology for preparing prednisolone acetate and enzymatic method, which is applied in the field of enzymatic preparation of steroidal anti-inflammatory drug prednisolone acetate, can solve the problems of low conversion rate, difficult extraction and purification, long conversion period and other problems of microbial conversion method, and achieves The effect of less enzyme dosage, good purity and high substrate concentration
CN105779552AInactive Publication Date: 2016-07-20ENZYMEWORKS
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
ENZYMEWORKS
Publication Date
2016-07-20
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a method for preparing steroid anti-inflammatory medicine prednisolone acetate by adopting an enzyme process. A compound 2 is taken as a substrate, the substrate reacts to generate a target product prednisolone acetate in presence of a hydrogen acceptor, a cosolvent and steroid 1,2-dehydrogenase, and the reaction is carried out in an aqueous phase buffer solution with the pH value of 5-9 and at the temperature of 10-45 DEG C, wherein the cosolvent is one or combination of more of dimethyl sulfoxide, Tween 60, Triton X 100 and polyethylene glycol, and the feeding volume of the cosolvent is 5-20% of the total volume of a reaction system. When the method disclosed by the invention is adopted for preparing the prednisolone acetate, the substrate concentration is high, the usage amount of enzyme is less, the operation is simple, the purity is high, and the conversion ratio is high.
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Description

technical field

[0001] The invention relates to the technical field of biochemical industry, in particular to a method for enzymatically preparing steroidal anti-inflammatory drug prednisolone acetate. Background technique

[0002] Prednisolone acetate (compound 1, also known as Prednisolone acetate) is an important adrenal glucocorticoid drug, mainly used for allergic and autoimmune inflammatory diseases, collagen diseases. Such as rheumatism, rheumatoid arthritis, lupus erythematosus, severe bronchial asthma, nephrotic syndrome, thrombocytopenic purpura, neutropenia, acute lymphoblastic leukemia, various adrenal insufficiency, exfoliative dermatitis, no blisters Sore neurodermatitis, eczema, etc.

[0003]

[0004] At present, prednisolone acetate can be obtained by prednisolone esterification (CN201510115790), and other synthetic techniques have microbial conversion and chemical synthesis two types of methods, and common routes are as follows:

[0005] 1. Chemical syn...

Claims

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