Preparation method of cyano reductase and gabapentin

A gabapentin and reductase technology, applied in biochemical equipment and methods, enzymes, enzymes, etc., can solve the problems of high risk factor, expensive, low efficiency, etc., achieve mild reaction conditions, increase overall yield, and reduce reaction steps Effect
CN113234698AActive Publication Date: 2021-08-10SHENZHEN READLINE BIOTECH CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
SHENZHEN READLINE BIOTECH CO LTD
Publication Date
2021-08-10

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Abstract

The invention relates to the technical field of medicine synthesis, in particular to a preparation method of cyano reductase and gabapentin. The method comprises the following steps: by taking sodium hydride as a catalyst, carrying out condensation reaction on cyclohexyl methyl cyanide and 2-ethyl bromoacetate to generate 2-cyano-2-cyclohexyl ethyl acetate; under an alkaline condition, carrying out hydrolysis reaction on 2-cyano-2-cyclohexyl ethyl acetate to obtain 2-cyano-2-cyclohexyl acetic acid; and converting the 2-cyano-2-cyclohexyl acetic acid into gabapentin under the action of the cyano reductase. Aiming at the defects (the problem of traditional chemical preparation of gabapentin) of a literature scheme, cyano reductase is introduced, and a route is systematically optimized, so that reaction steps are reduced, and meanwhile, reaction conditions are milder and more environment-friendly. According to the route, the overall yield of gabapentin can be remarkably increased, and meanwhile, the gabapentin better meets the requirements of current green production.
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Description

technical field

[0001] The invention relates to the technical field of drug synthesis, in particular to a preparation method of gabapentin. Background technique

[0002] Gabapentin is a drug for the treatment of partial epilepsy, and it is also the drug of choice for the treatment of neuropathic pain such as diabetic neuritis and post-herpetic severe pain.

[0003] Traditional gabapentin preparation method is as follows:

[0004]

[0005] Route I: This preparation method has been reported in many articles and patents, Dipak Varal et al {Chem.Sci.Trans, 5,442-446 (2016)}, Ashok Kumar mubai et al (Patent US20080103334A1), Delogu Pietro et al (Patent EP 2368872A1), Wolfram Geibel et al. (Patent US005091567A). Cyclohexanone is first condensed with ethyl cyanoacetate, then hydrolyzed under strong acid and high temperature, acetic anhydride forms ester, ammonolysis, and finally Hofmann rearranges five steps to obtain gabapentin;

[0006] Route II: People such as Gareth Griff...

Claims

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