Process for the preparation of ceftriaxon disodium salt hemihept

Details Process for the preparation of ceftriaxon disodium salt hemihept Process for the preparation of ceftriaxon disodium salt hemihept

1993-01-27

1996-06-18

Rizzo, Nicholas

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

540226, C07D50136

Patent

active

055279066

ABSTRACT:
A new and improved process for the preparation of ceftriaxon disodium salt hemiheptahydrate of formula I ##STR1## is described, wherein 7-amino-3-{[(2,5-dihydro-6-hydroxy-2-methyl-5-oxo-as-triazin-3-yl)thio]met hyl}-3-cephem-4-carboxylic acid disodium salt is converted with a reactive 2-(2-aminothiazol-4-yl)-2-syn-metoxyimino acetic acid derivative such as 2-benzo-thiazolyl-thio ester in a water solution and in the presence of a suitable inert organic solvent such as acetone, at a temperature between 0.degree. C. and 40.degree. C. and then the desired compound is isolated in a very pure form and with a high total yield.
Ceftriaxon is a cephalosporin antibiotic of the third generation for parenteral application and a valuable agent for the treatment of heavy infections.

REFERENCES:
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patent: 4758556 (1988-07-01), Durckheimer et al.
patent: 4767852 (1988-08-01), Ascher
patent: 5026843 (1991-06-01), Riccardo et al.
patent: 5126445 (1992-06-01), Martin
An Encyclopedia of Chemicals, Drugs, and Biologicals, The Merck Index, Eleventh Edition, Merck & Co., Inc., Rahway, New Jersey, pp. 294-301, 165,166. (1989).

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