Method for preparing moxifloxacin side chain through biological method

A technology of compound and transaminase, which is applied in the production of bulk chemicals, organic chemistry, fermentation, etc., can solve the problems of long nonane steps, high environmental pressure, and unknown enzyme sources, etc.
CN106399418AActive Publication Date: 2017-02-15ENZYMEWORKS
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
ENZYMEWORKS
Publication Date
2017-02-15

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Abstract

The present invention provides a method for preparing a moxifloxacin side chain through a biological method, particularly to a method for preparing a compound represented by a formula 2. The method comprises: catalyzing a compound represented by a formula 4 with transaminase to form a compound represented by formula 3, and carrying out spontaneous ring closure on the compound represented by the formula 3 to obtain the compound represented by the formula 2, wherein the transaminase is selected from the omega-transaminase in Arthrobacter, Aspergillus terreus, Vibrio fluvialis, Bacillus megaterium, Sphingomonas paucimobilis, Hyphomonasneptunium, and Chromobacterium violaceum, and in the formulas 2, 3 and 4, R is selected from benzyloxycarbonyl, benzyl and ethoxycarbonyl. The formulas 2, 3 and 4 are defined in the specification.
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Description

technical field

[0001] The invention belongs to the technical fields of biopharmaceuticals and biochemical engineering, and in particular relates to a production method for preparing moxifloxacin side chains by a biological method. Background technique

[0002] (S,S)-2,8-Diazabicyclo[4.3.0]nonane(1) and its N-protected derivative(2) are key chiralities for the synthesis of widely used quinolone antibacterial drug moxifloxacin Intermediate, also known as moxifloxacin side chain or moxi small ring:

[0003]

[0004] Since (S,S)-2,8-diazabicyclo[4.3.0]nonane contains two chiral centers, its synthesis methods usually include resolution method, asymmetric synthesis method and chiral source method. The resolution method is the most important application method. Using pyridine 2,3-dicarboxylate as the starting material, the racemate of benzyl-protected 1 is obtained by high-pressure hydrogenation and other methods, and the product is obtained by resolution using tartaric acid a...

Claims

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