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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

Inactive Publication Date: 2016-07-20
ENZYMEWORKS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The conversion rate of the microbial conversion method is low, generally not more than 70%, the conversion period is long (more than 60 hours), the extraction and purification after conversion is difficult, and the result is unstable

Method used

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

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Embodiment 1 (screening of enzyme):

[0023] Compound 210mg was added to 1.55mL pH7.0 phosphate buffered saline solution, then 200 μl mass fraction of 10% DMSO, 100 μl mass fraction of 5% Tween-60, 150 μl 60 mg / ml menadione aqueous solution, and steroid Body 1,2 dehydrogenase (purchased from Suzhou Hanzyme Biotechnology Co., Ltd.) 10 mg, shaken at 30 ° C for 2 h, and the conversion rate was detected, as shown in Table 1.

[0024] Table 1

[0025] enzyme

[0026] It can be seen from Table 1 that, under other conditions being the same, when the steroidal 1,2 dehydrogenase brand EW1147 is selected, the conversion rate is the highest.

Embodiment 2

[0027] Embodiment 2 (scale-up preparation):

[0028] Dissolve 220g of the compound in 20mL of DMSO, add it into 30mL of pH8.00.1M phosphate buffer solution dissolved with 2.5mL of Tween 60, then add 75g of steroidal 1,2 dehydrogenase EW11475g, 10g of naphthoquinone, shake at 35°C for 12h , adopt HPLC to detect that the conversion rate of compound 2 is 100%, then centrifuge at 10000g for 10min, discard the supernatant, add 50mL chloroform to wash the precipitate, filter, and rotary steam to obtain product prednisolone acetate 19.5g, purity 95%, conversion rate was 93.1%.

[0029] The conversion rate analysis method is as follows:

[0030] HPLC (Shimadzu LC-2010) is equipped with sepaxBR-C18 chromatographic column (4.6*150mm, 5μm), mobile phase: 0-12min, 40% acetonitrile, 60% water, flow rate 1mL / min, detection wavelength 244nm, column temperature 30 The peak time is: 8.3 minutes for the substrate and 7.6 minutes for the product.

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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.

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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Application Information

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IPC IPC(8): C12P33/02
CPCC12P33/02
Inventor 梁晓亮李国庆
Owner ENZYMEWORKS
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