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Synthetic technology of cefditoren pivoxil intermediate

A cefditoren pivoxil and synthetic process technology, applied in the direction of organic chemistry, etc., can solve the problems of long synthetic steps, environmental pollution, difficult to handle by-product chromium salts, etc., and achieve mild reaction conditions, easy post-treatment, and simple operation Effect

Inactive Publication Date: 2012-05-16
王颢
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the main disadvantage of the PDC oxidation method is that the by-product chromium salt is difficult to handle, which is easy to cause environmental pollution; the synthesis steps of the NBS method are long and do not have atom economy; the raw materials of the thiazole carbonitrile reduction method are not easy to obtain

Method used

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  • Synthetic technology of cefditoren pivoxil intermediate
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  • Synthetic technology of cefditoren pivoxil intermediate

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Experimental program
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Effect test

Embodiment Construction

[0020] Processing step of the present invention is:

[0021] 1. Preparation of methyl 2-amino-4-methyl-5-thiazolecarboxylate

[0022] The reaction equation is:

[0023]

[0024] 2. Preparation of methyl 4-methyl-5-thiazolecarboxylate

[0025] The reaction equation is:

[0026]

[0027] 3. Preparation of 4-methyl-5-formylthiazole

[0028] The reaction equation is:

[0029]

[0030] The product of the present invention has been confirmed by nuclear magnetic spectrum and mass spectrogram.

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Abstract

The invention which belongs to the medicine processing field concretely relates to a synthetic technology of a cefditoren pivoxil intermediate. The synthetic technology of the cefditoren pivoxil intermediate provided in the invention has the advantages of simple operation, no pollution and high yield. The technology of the invention comprises the following steps: preparation of 2-amino-4-methyl-5-methylthiazole formate, preparation of 4-methyl-5-methylthiazole formate and preparation of 4-methyl-5-formylthiazole.

Description

Technical field: [0001] The invention belongs to the field of medicine processing, and more specifically relates to a synthesis process of a cefditoren pivoxil intermediate. Background technique: [0002] 4-Methyl-5-formylthiazole is an important side chain for the synthesis of the third-generation cephalosporin antibacterial drug cefditoren pivoxil, and their molecular structures are shown in the figure below. [0003] [0004] 4-Methyl-5-formylthiazole Cefditoren pivoxil [0005] There are many synthetic pathways for 4-methyl-5-formylthiazole, which are mainly divided into two categories: (1) Synthesis from 4-methyl-5-thiazole formic acid ester. The method can be divided into: catalytic hydrogenation method, hydrazine hydrate reduction method and reduction oxidation method. ZrO for catalytic hydrogenation 2 As a catalyst, high temperature and high pressure reaction, the conditions are relatively harsh, the yield is medium, and it is difficult to realize industrializa...

Claims

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Application Information

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IPC IPC(8): C07D277/24
Inventor 王颢
Owner 王颢
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