摘要:
A 7-Acylamino-3-methyl-3-cephem-4-carboxylic acid is prepared by first forming a 7-acylamino-3-methyl-3-cephem-4-carboxylic acid ester by heating a 6-acyl-aminopenicillanic acid ester S-oxide in the presence of a catalyst consisting of an acid and a sulfide and then deesterifying the intermediate 7-acylamino-3-methyl-3cephem-4-carboxylic acid ester.
摘要:
The invention is concerned with two novel crystalline forms of the antibiotic cephaloridine which are relatively non-hygroscopic compared with previously known forms of cephaloridine and hence possess important advantages in handling and formulation. The novel crystalline forms are characterised in particular by X-ray crystallographic data set out in detail in the following disclosure.
摘要:
3-( Alpha -Trifluoromethylarylacetamido)-1,4-(cyclo-(1''carboxy)alkylenethio)azetidin-2-one derivatives possessing antibacterial activity are produced by the reaction of 3,3,3trifluoro-2-phenylpropanoic acid or 3,3,3-trifluoro-2-phydroxyphenylpropanoic acid and a 3-amino-1,4-(cyclo(1''carboxy)alkylenethio)-azetidin-2-one derivative in the presence of a condensing agent or by conversion of the propanoic acid derivative to an acid halide.
摘要:
Novel 6-APA, 7-ACA, and 7-ADCA derivatives are described which comprise phosphorylated derivatives of 6-APA, 7-ACA, or 7-ADCA and the corresponding acylated derivatives thereof. The novel compounds are prepared by the reaction of 6-APA, 7-ACA, 7-ADCA or a salt thereof with a phosphorus halide in the presence of an acid acceptor and subsequently acylating the thus formed phosphorylated compound, to form a phosphorylated acylated derivative which upon hydrolysis with water splits off the protective group(s) to provide the corresponding semi-synthetic penicillin or cephalosporin having useful antibacterial activity.
摘要:
A process is provided which yields derivatives of cephalosporins and penicillins. The process starts with 7-aminodecephalosporanic acid or 6-APA and reacts with a carbonyl containing compound to form a Schiff''s base (imino) adduct. This latter compound is then treated with a defined reagent yielding a novel Schiff''s base adduct having a side chain on the carbon adjacent to the iminonitrogen. The amino moiety can be regenerated and further reacted to form end compounds which are active against both gram-positive and gram-negative bacteria.