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.
CN102443013AActive Publication Date: 2012-05-09CSPC MEGALITH BIOPHARMACEUTICAL CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
CSPC MEGALITH BIOPHARMACEUTICAL CO LTD
Publication Date
2012-05-09

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Abstract

The invention relates to an improved method for preparing a cefprozil dimethyl formamide (DMF) solvate; the method comprises the following steps of: taking a 7-APCA-guanidine salt shown by the formula IV and a mixed anhydride shown by the formula VI as raw materials to carry out a condensation reaction under alkaline conditions, hydrolyzing reaction liquid in the presence of acids, separating the liquid, adding DMF to a water phase, and regulating a pH value with an alkaline to obtain the cefprozil DMF solvate shown by the formula I. The method of the invention avoids the usage of silanizing reagent with expensive cost and instability, improves yield greatly and reduces production cost to form a more economic and efficient preparation technology, wherein X+ and R6 are defined according to claim 1.
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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

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