Process for preparing cephalosporin derivatives

Details Process for preparing cephalosporin derivatives Process for preparing cephalosporin derivatives

1983-12-02

1985-10-15

Rizzo, Nicholas S.

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

Organic compounds

Chalcogen in the nitrogen containing substituent

544 28, 544 22, C07D50114, A61K 31545

Patent

active

045475733

ABSTRACT:
A process for the manufacture of a cephalosporin derivative of the formula I ##STR1## in which X is sulphur, oxygen or sulphinyl; R.sup.1 is any one of the C-3 substituents from antibacterially-active cephalosporins known in the art; R.sup.2 is hydrogen or 1-6C alkyl; R.sup.3 is hydrogen or 1-6C alkyl; and the pharmaceutically-acceptable acid-addition and base-addition salts thereof, characterized by cyclization of a compound of the formula II: ##STR2## or a derivative thereof in which the carbonyl group is masked, or an acid-addition salt thereof, in which R.sup.4 and R.sup.5 individually have one of the values for R.sup.2 and R.sup.3, R.sup.6 is a nitrogen-protecting group and R.sup.7 is hydrogen or any one of the cephalosporin 3-carboxylic acid protecting groups known in the art;
whereafter when the product from the cyclization retains the protecting group R.sup.7 (when R.sup.7 is other than hydrogen) the protecting group R.sup.7 is replaced by hydrogen by conventional means;
and whereafter when the compound of the formula I is obtained in the form of the free base or salt, and a pharmaceutically-acceptable salt or free base respectively is required, any necessary conversion between free base and salt is carried out by conventional means.

REFERENCES:
patent: 4463173 (1984-07-01), Jung
patent: 4490382 (1984-12-01), Jung et al.

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