http://rdf.ncbi.nlm.nih.gov/pubchem/patent/GB-1462944-A
Outgoing Links
Predicate | Object |
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assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_2ca2e4410855da087e11bf3eea8933fa |
classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/Y02P20-55 |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D501-20 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D501-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D501-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-04 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D501-59 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07B61-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D501-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D501-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-546 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-545 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D501-20 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P31-04 |
filingDate | 1974-03-07-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationDate | 1977-01-26-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | GB-1462944-A |
titleOfInvention | Process for preparing cephalosporins |
abstract | 1462944 3-Fluoro-cephem derivatives ELI LILLY & CO 7 March 1974 [6 Feb 1974] 10352/74 Heading C2C Compounds of the Formula (I) where R is an acyl group R<SP>1</SP>CO-, wherein R<SP>1</SP> is C 1-6 alkyl, C 1-3 halalkyl, C 1-3 cyanalkyl, phenyl, methylphenyl, hydroxyphenyl, halophenyl, nitrophenyl, methoxyphenyl or a group of the formula wherein A is diphenylmethyl, p-nitrobenzyl, benzyl, 2,2,2-trichloroethyl, t-butyl, or pmethoxybenzyl and A<SP>1</SP> is C 2-4 alkanoyl, C 2-4 haloalkanoyl, benzoyl, halobenzoyl, 2,4-dinitrophenyl or phthaloyl; or R<SP>1</SP> is a group of the formula wherein a and a<SP>1</SP> independently are H, C 1-4 alkyl, C 1-4 alkoxy, halogen, hydroxy, or nitro; Z is O or S; and m is 0 or 1; or R<SP>1</SP> is a group of the formula wherein P is 2- or 3-thienyl, or a phenyl group of the formula where Q is OH, formyloxy, acetoxy, amino or protected amino; or R<SP>1</SP> is R<SP>11</SP>CH 2 -, where R<SP>11</SP> is 2- or 3-thienyl, 2-furyl, 2-oxazyl, 2-thiazyl or 1-tetrazyl; and R 1 is H, benzyl, p-methoxybenzyl, p-nitrobenzyl, diphenylmethyl, 2,2,2- trichloroethyl, or t-butyl; are prepared by reacting a 3-sulphonate ester cephalosporin of the Formula (II) wherein R 1 is a carboxylic acid protecting ester forming group and W is C 1-6 alkyl, phenyl, tolyl, halophenyl or nitrophenyl, with an inorganic fluoride M<SP>+</SP>F<SP>-</SP> in which M is K<SP>+</SP>, Na<SP>+</SP> or Ag<SP>+</SP> in the presence of an 18-crown-6 ether and an inert solvent at a temperature of - 20 to + 25 C.; and if desired removing the carboxylic acid protecting ester forming group and, if desired, any amine-protecting group, to provide the corresponding acid. Intermediate p - nitrobenzyl 7 - [2 - (2- thienyl)acetamido] - 3 - methylsulphonyloxy - 3- cephem - 4 - carboxylate is obtained by reacting the corresponding 3-hydroxy-3-cephem compound with methane sulphonyl chloride. This method is also described more generally. |
priorityDate | 1974-02-06-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 44.