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Method for preparing steroidanti-inflammatory drugintermediatetetraene acetate using enzyme process

A technology for the preparation of tetraenyl acetate and enzymatic method, which is applied in the field of tetraenyl acetate, an intermediate of steroid anti-inflammatory drugs, can solve the problems of low concentration of reaction substrate, complicated product separation, unfriendly environment, etc., and achieve production Low cost, simple preparation steps, and environmentally friendly effects

Inactive Publication Date: 2016-05-04
ENZYMEWORKS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The object of the present invention is to provide a kind of method that enzymatically prepares steroidal anti-inflammatory drug intermediate acetate tetraenyl thing, overcomes the step complexity that adopts chemical method to exist in the process of steroidal anti-inflammatory drug intermediate preparation in the prior art by this method, The environmental unfriendly problems caused by the use of a large amount of organic solvents and metal catalysts; at the same time, it overcomes the problems of low concentration of reaction substrate and complicated separation of products in the preparation process of fermentation method

Method used

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  • Method for preparing steroidanti-inflammatory drugintermediatetetraene acetate using enzyme process
  • Method for preparing steroidanti-inflammatory drugintermediatetetraene acetate using enzyme process
  • Method for preparing steroidanti-inflammatory drugintermediatetetraene acetate using enzyme process

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Example 1 Screening of steroidal 1,2 dehydrogenase

[0024] Add 10 mg of compound II to 2 mL of pH 7.0 phosphate buffer solution, then add 10 mg of steroid 1,2 dehydrogenase of different brands purchased from Suzhou Hanzyme Biotechnology Co., Ltd., shake at 30 °C for 2 h, and detect The conversion rate of the substrate is shown in Table 1.

[0025] Table 1

[0026] enzyme

[0027] It can be seen from Table 1 that, under other conditions being the same, when the steroidal 1,2 dehydrogenase with brand name EW1145 is used as the steroidal 1,2 dehydrogenase, the conversion rate of the substrate is the highest.

Embodiment 2

[0028] Substrate conversion rate situation under the different temperature conditions of embodiment 2

[0029] Add 10 mg of compound II to 2 mL of pH 7.0 phosphate buffer solution, add 1 mg of steroidal 1,2 dehydrogenase (purchased from Suzhou Hanzyme Biotechnology Co., Ltd., brand EW1145, the same below), under different temperature conditions , shaken for 12 hours, and the conversion rate of the detected substrate is shown in Table 2.

[0030] Table 2

[0031] temperature °C

[0032] It can be seen from Table 2 that, under other conditions being the same, the conversion rate of compound II is the highest when the reaction temperature is controlled at 30°C.

Embodiment 3

[0033] Substrate conversion rate situation under the different pH conditions of embodiment 3

[0034] Add 10mg of compound II to 2mL of phosphate buffer solution with different pH, add 1mg of steroidal 1,2 dehydrogenase, shake and react at 30°C for 12h, and detect the conversion rate of the substrate as shown in Table 3.

[0035] table 3

[0036] pH

[0037] As can be seen from Table 3, under other conditions being the same, the conversion rate of the substrate is the highest when the above reaction is carried out in a buffer solution with a pH of 7.0.

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Abstract

The invention discloses a method for preparing steroidanti-inflammatory drugintermediatetetraene acetate using an enzyme process. In the method, a compound II serves as a reaction substrate and experiences reactions in a buffer solution with pH 6.0-8.0 at 15-30 DEG EC under the effect of steroid 1,2-dehydrogenase to generate a steroidanti-inflammatory drugintermediate I. The method solves the problem that preparation of a steroidanti-inflammatory drugintermediate using an enzyme process is unavailable in the prior art; and compared with traditional methods, the method has the advantages of high substrate concentration, low enzyme consumption, simple preparation steps, environmental friendliness and low production cost and is suitable for large-scale production.

Description

technical field [0001] The invention relates to the technical fields of biological pharmacy and biochemical industry, in particular to a method for enzymatically preparing tetraenyl acetate, an intermediate of steroidal anti-inflammatory drugs. Background technique [0002] Acetate tetraene (compound I, has another name called teraene, 3TR), its structural formula is: Tetraenyl acetate can be prepared as an intermediate to obtain a variety of steroidal compounds with good anti-inflammatory effects, such as triamcinolone acetonide (TriamcinoloneAcetonide), prednisolone (trade name Donison) and dexamethasone (Dexamethasone) etc., these drugs are in There are extensive and a large number of clinical applications (Bioorganic & Medicinal Chemistry 21 (2013) 2241–2249, Steroids 78 (2013) 1281–1287, etc.). [0003] Patents CN201210038066, 200910070841 and literature Steroids78 (2013) 1281-1287 disclose several chemical methods for preparing compound I, which usually require multi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C12P33/02
CPCC12P33/02
Inventor 陶军华梁晓亮杨锴
Owner ENZYMEWORKS
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