| 摘要 |
1336328 Salts of penicillins and cephalosporins CHEMIE GRUNENTHAL GmbH 25 May 1971 [30 May 1970 (3) 31 March 1971] 16928/71 Heading C2A A process for preparing salts of carboxylic acids which contain a #-lactam ring comprises reacting a silylderivative of a penicillin, cephalosporin or of 6-aminopenioillanic acid, in which at least the carboxyl group is attached to a group derived from a trialkyl or triaryl silanol or from a dialkyl or diaryl silane diol through the silicon atom thereof, in the presence of an aprotic organic solvent with a compound of Formula I: in which R 1 represents an acyl radical derived from a carboxylic acid which does not contain any ionizable proton groups, an alkyl radical or an aryl radical or a group of Formula II: in which R 2 , R 3 and R 4 may be the same or different and each represents an alkyl or aryl radical, and Cat represents a cation. The above reaction may be carried out in the presence of an amount of water or an alcohol insufficient for desilylating the silyl derivative of the carboxylic acid containing a #-lactam ring. The silyl derivative may be a penicillin of Formula III: in which X represents an acyl radical, Y represents a group derived from a trialkyl or triaryl silanol or from a dialkyl or a diaryl silane diol and attached through a silicon atom, and Z represents a hydrogen atom or has the same meaning as Y. X may be, for example, the radical ofα-phenoxyacetic, propionic or butyric acid; anα-amino,α-halogeno orα-alkoxyphenylacetic acid; a 3- (or 5-) aryl-5- (or 3-) alkylisoxazolyl-4-carboxylic acid or of 1-aminocyclohexane-1-carboxylic acid. Also, salts of penicillins, cephalosporins or 6-aminopenicillanic acid may be prepared by the above procedures. |
