ES380395A1 - Procedure for the obtaining of derivatives of the acid 7- aminocefalosporanico. (Machine-translation by Google Translate, not legally binding) - Google Patents

Abstract

Procedure for obtaining derivatives of 7-aminocephalosporanic acid, of formula **(See formula)** where R is hydrogen or a hydroxyl group esterified by a carboxylic acid, the oxygen atoms of the ester group being able to be substituted by sulfur atoms, but not the acetoxy group, a carbamoyloxy group in given N-substituted cases where oxygen atoms can be replaced by sulfur atoms, or a quaternary amino group and in certain cases its internal salts. It is characterized in that compounds of formula II are reacted with a metal azide **(See formula)** where Z is a reactable esterified hydroxyacetyl moiety and R is hydrogen or a free or esterified hydroxyl group (where in the ester group oxygen atoms can be replaced by sulfur atoms); Acylated with the group N3CH2-CO- is a compound of formula II, where Z is hydrogen and R is hydrogen or a free or esterified hydroxyl group (where the oxygen atoms of the ester group can be replaced by sulfur atoms); of compounds of formula I, where the carboxyl group is protected by an easily separable group, this group is cleaved, and the obtained compounds, in which R is the acetoxy group, are transformed into compounds with free hydroxyl group or quaternary amino group R and compounds with free hydroxyl group R are transformed into compounds containing another ester group other than acetoxy (in where in given cases the oxygen atoms can be replaced by sulfur atoms) or in a carbamoyloxy group, in given N-substituted cases in which the oxygen atoms can be substituted into sulfur atoms. If desired in the compounds obtained, in which R represents a hydroxyl group esterified by a carboxylic acid except for acetic acid, this group is replaced by a quaternary amino group and in given cases, if desired, the combinations obtained are transformed into its metallic salts for therapeutic use such as those of alkali or alkaline earth metals, or salts with ammonia or organic bases, or from the salts obtained free carboxylic acids are formed or, in certain cases, their internal salts. (Machine-translation by Google Translate, not legally binding)