Process for the manufacture of cephalosporin derivatives

Details Process for the manufacture of cephalosporin derivatives Process for the manufacture of cephalosporin derivatives

1982-06-14

1985-02-05

Rizzo, Nicholas S.

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

Organic compounds

Chalcogen in the nitrogen containing substituent

544 28, 544 22, 544 26, C07D50136, A61K 31425

Patent

active

044979495

ABSTRACT:
The invention relates to a process for the manufacture of a cephalosporin derivative of the formula I: ##STR1## in which X is a sulphur or oxygen atom or a sulphinyl radical, R.sup.1 is any one of the C-3 substituents from antibacterially-active cephalosporins known in the art, R.sup.2 is a hydrogen atom or a 1-6C alkyl or 2-6C alkenyl radical, R.sup.3 is a hydrogen atom or one of a variety of radicals defined in the specification, and the pharmaceutically-acceptable acid- and base-addition salts thereof, characterized by reaction of a compound of the formula IX: ##STR2## in which R.sup.16 and R.sup.17 individually have one of the values given above for R.sup.2 and R.sup.3, or a derivative thereof in which the carbonyl group is masked, with a compound of the formula X: ##STR3## in which R.sup.18 is a hydrogen atom or any one of the cephalosporin 3-carboxylic acid protecting groups known in the art; whereafter, when R.sup.18 is other than a hydrogen atom, the protecting group R.sup.18 is replaced by hydrogen by conventional means.

REFERENCES:
patent: 2331671 (1943-10-01), Ericks
patent: 4358447 (1982-11-01), Hannah
J. Chem. Soc., 1956, 307-310.
J. Amer. Chem. Soc., 1955, 77, 1056.

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