http://rdf.ncbi.nlm.nih.gov/pubchem/patent/GB-1297069-A
Outgoing Links
| Predicate | Object |
|---|---|
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D501-38 |
| classificationIPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-545 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D501-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D501-44 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D501-38 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A23K20-195 |
| filingDate | 1970-04-21-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 1972-11-22-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | GB-1297069-A |
| abstract | 1297069 Cephalosporin derivatives BRISTOLMYERS CO 21 April 1970 [21 April 1969] 19062/70 Headings C2A and C2C Cephalosporin derivatives having the Formula I: wherein Ar is 2-thienyl, 3-thienyl or in which each of R<SP>1</SP> and R<SP>2</SP> is H, NO 2 , di-C 1-6 - alkylamino, C 1-6 alkanoylamino, amino, hydroxy, C 1-6 alkanoyloxy, C 1-6 alkyl, C 1-6 alkoxy, sulphamyl, Cl, I, Br, F or trifluoromethyl and non-toxic pharmaceutically acceptable salts thereof may be prepared by hydrolysing a compound having the Formula II: or a non-toxic salt thereof in the presence of an acid to remove the t-butoxycarhonyl functional group. The starting material of Formula II may be prepared by (1) acylating 7-amino-3- azidomethylceph-3-em-4-oic acid or a non-toxic salt thereof with an equimolar weight of an acid having the Formula III: or with a functional equivalent thereof in an inert solvent at a temperature below 5‹ C., or (2) acylating 7-amino-cephalosporanic acid or a non-toxic salt thereof with an equimolar weight of an acid having Formula III or with a functional equivalent thereof in an inert solvent at a temperature below 5‹ C. to form an intermediate having the formula or a non-toxic salt thereof and reacting the intermediate with sodium azide, in the presence of a base, in aqueous solvent. Preferably the acid hydrolysis reaction comprises treating the compound of Formula II with an excess of 40 to 60% aqueous formic acid or concentrated trifluoroacetic acid. The non-toxic pharmaceutically acceptable salts include Na, K, Ca, A1 and ammonium salts, substituted ammonium salts with amines and acid addition salts with mineral and organic acids. Antibacterial pharmaceutical compositions comprise compounds of Formula I and a diluent or carrier. The acids of Formula III wherein Ar is as defined above are prepared by reacting the corresponding acid having a free amino radical with t-butoxy carbonyl azide. |
| isCitedBy | http://rdf.ncbi.nlm.nih.gov/pubchem/patent/FR-2215942-A1 |
| priorityDate | 1969-04-21-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 30.