C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/100
C07D 498/04 (2006.01) C07D 309/14 (2006.01) C07D 501/18 (2006.01) C07D 501/59 (2006.01) C07D 505/00 (2006.01) C07F 7/10 (2006.01)
Patent
CA 1203235
Abstract PROCESS A process for the manufacture of a cephalosporin derivative of the formula I:- Image I in which X is sulphur, oxygen or sulphinyl; R1 is any one of the C-3 substituents from antibacterially-active cephalosporins known in the art; R2 is hydrogen or 1-6C alkyl; R3 is hydrogen or 1-6C alkyl; and the pharmaceutically-acceptable acid-addition and base- addition salts thereof, characterised by cyclisation of a compound of the formula II:- Image II or a derivative thereof in which the carbonyl group is masked, or an acid-addition salt thereof, in which R4 and R5 individually have one of the values for R2 and R3, R6 is a nitrogen-protecting group and R7 is hydrogen or any one of the cephalosporin 3-carboxylic acid protecting groups known in the art; whereafter when the product from the cyclisation retains the protecting group R7 (when R7 is other than hydrogen) the protecting group R7 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.
443481
Jung Frederic H.
Loftus Frank
Olivier Annie A.
Ballantyne Donald G.
I.c.i Pharma
Imperial Chemical Industries Plc
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