Method for preparing cefprozil dimethyl formamide solvate

A technology of propylene dimethyl formamide and solvate, which is applied in the field of preparation of important intermediates of antibiotics, and can solve the problems of high price and unstable silylating reagents, etc.
CN102443013BActive Publication Date: 2014-09-17CSPC MEGALITH BIOPHARMACEUTICAL CO LTD
6 Cites 0 Cited by

Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
CSPC MEGALITH BIOPHARMACEUTICAL CO LTD
Publication Date
2014-09-17

Smart Images

  • Figure 1
    Figure 1
  • Figure 2
    Figure 2
  • Figure 3
    Figure 3
Patent Text Reader

Abstract

The present invention relates to an improved method for preparing cefprozil dimethylformamide solvate, the method is to use 7-APCA-guanidine salt shown in formula IV and mixed anhydride shown in formula VI as raw materials under alkaline conditions Condensation reaction is carried out, the obtained reaction solution is hydrolyzed in the presence of an acid, the liquid is separated, DMF is added to the water phase, and the pH value is adjusted with alkali to obtain the cefprozil DMF solvate shown in formula I. The method of the invention avoids the use of expensive and unstable silylating reagents, greatly improves the product yield, reduces production costs, and is a more economical and effective preparation process. Wherein, X+, R6 are as defined in claim 1.
Need to check novelty before this filing date? Find Prior Art

Description

technical field

[0001] The present invention relates to a kind of preparation method of important intermediate of antibiotics, in particular to a kind of preparation method of cefprozil dimethylformamide solvate (hereinafter referred to as cefprozil DMF solvate) shown in formula I.

[0002] Background technique

[0003] The chemical name of cefprozil is (6R,7R)-7-[2-amino-2-(4-hydroxyphenyl)acetamido]-3-[(Z)-propenyl]-3-cephem-4- Carboxylic acid, which is a monohydrate for medicinal use (the structural formula is shown in formula II). This substance is a cephalosporin broad-spectrum antibacterial drug developed by Bristol-Myers Squibb Company of the United States. + , G - Bacteria and anaerobic bacteria have strong antibacterial activity, against G + Bacteria are particularly prominent.

[0004]

[0005] Cefprozil DMF solvate is an important intermediate in the synthesis of cefprozil.

[0006] In U.S. Patents US20040087786, US20090048460, Chinese patents CN1694888...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More