Synthesis method for moxifloxacin side chain

A moxifloxacin side chain and synthesis method technology, applied in the direction of organic chemistry, can solve the problems of many operation steps, environmental pollution, high cost, etc., and achieve the effect of reducing industrial waste, reducing production cost, and improving productivity

Inactive Publication Date: 2016-07-20
江西中德诚信科技有限公司 +1
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Problems solved by technology

Now the difficulty of synthesis is that the synthesis process of moxifloxacin side chain is complicated. The common synthetic route of the prior art is to carry out chemical reduction first, and then split to obtain the yield of moxifloxacin side chain is lower than 45%, and there are many operation steps and cost High, serious environmental pollution

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  • Synthesis method for moxifloxacin side chain

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Embodiment Construction

[0022] The following is a clear and complete description of the technical solutions in the embodiments of the present invention. Apparently, the described embodiments are only some of the embodiments of the present invention, not all of them. Based on the embodiments of the present invention, all other embodiments obtained by persons of ordinary skill in the art without making creative efforts belong to the protection scope of the present invention.

[0023] The embodiment of the present invention discloses a method for synthesizing moxifloxacin side chains with less industrial waste, low production cost and high productivity, using 2,3-pyridinedicarboxylic acid as raw material, through cyclization, catalytic hydrogenation, resolution, Racemization, chemical reduction, debenzylation to obtain moxifloxacin side chain, the specific synthesis method is:

[0024] S1, ring closure:

[0025] Add 120g of 2,3-pyridinedicarboxylic acid and 110g of acetic anhydride into the flask, stir...

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Abstract

The invention discloses a synthesis method for a moxifloxacin side chain.With 2,3-dipicolinic acid being a raw material, cyclization, catalytic hydrogenation, resolution and racemization are performed, and then chemical reduction and debenzylation are performed to obtain moxifloxacin side chain.Resolution, racemization and chemical reduction are performed in sequence, sodium borohydride is used for replacing high-risk lithium aluminum hydride to synthesize the moxifloxacin side chain, and the synthesis method has the advantages that industrial waste materials are reduced, the production cost is lowered, and productivity is increased.

Description

technical field [0001] The invention relates to the technical field of antibacterial drugs, in particular to a method for synthesizing moxifloxacin side chains. Background technique [0002] Moxifloxacin hydrochloride is a new type of 8-methoxy fluoroquinolone fourth-generation antibacterial drug developed by Bayer in Germany. It is a synthetic quinolone antibacterial drug. It is a newer synthetic antibacterial drug with strong antibacterial properties and a wide antibacterial spectrum , It is not easy to produce drug resistance and is effective against common drug-resistant bacteria, long half-life, and less adverse reactions. Moxifloxacin has many dosage forms, large market usage, and broad prospects. Now the difficulty of synthesis is that the synthesis process of moxifloxacin side chain is complicated. The common synthetic route of the prior art is to carry out chemical reduction first, and then split to obtain the yield of moxifloxacin side chain is lower than 45%, and ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D471/04
CPCC07D471/04
Inventor 喻理德张文锍徐诚
Owner 江西中德诚信科技有限公司
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