http://rdf.ncbi.nlm.nih.gov/pubchem/patent/GB-1377307-A
Outgoing Links
Predicate | Object |
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assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_76195fd1cd08192222699d8e7a88c231 |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D499-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07F9-4006 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07F9-65611 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D499-44 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D499-58 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07F9-40 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D499-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07F9-6561 |
filingDate | 1972-02-18-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationDate | 1974-12-11-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | GB-1377307-A |
titleOfInvention | Alpha-phosphonoacetylpenicillins |
abstract | 1377307 α - Phosphonoacetylpenicillins, phosphonic acids and esters thereof E R SQUIBB & SONS Inc 18 Feb 1972 [22 Feb 1971] 7741/72 Headings C2A and C2P The invention comprises α-phosphonoacetylpenicillins of Formula I wherein R is hydrogen, C 1 -C 8 alkyl, aralkyl, or a salt forming ion; R 1 is hydrogen, C 1 -C 8 alkyl, aralkyl, monocyclic carbocyclic aryl, or a monocyclic heterocyclic containing 5 or 6 members in the ring consisting of carbon, oxygen, nitrogen and sulphur, no more than two being other than carbon; R 2 and R 3 are each hydrogen, metal ion, amine salt ion, C 1 -C 8 alkyl, monocyclic carbocyclic aryl or aralkyl and R 4 is C 1 -C 8 alkyl, monocyclic carbocyclic aryl or aralkyl. A process, for preparing compounds of Formula I comprises reacting a 6-amino penicillanic acid of the Formula II: wherein R is as hereinbefore defined with an α- phosphonoacetic acid of Formula III: or an acylating derivative thereof. Pharmaceutical and disinfectant compositions having antibiotic properties may be prepared from compounds of Formula I in conjunction with suitable carriers. α-Phosphonophenylacetic acid- P,P-diethyl ester is prepared by reaction of benzylphosphonic acid diethyl ester (obtained by refluxing a solution of triethyl phosphite acid benzyl chloride) with carbon dioxide in the presence of butyl lithium. Hydrolysis yields the corresponding P-monoethyl ester and the free α-phosphonophenyl acetic acid. α-Phosphonophenyl acetic acid-P,P-dibenzyl ester and the corresponding P-monobenzyl ester may be similarly prepared. α-Phosphonophenylacetic acid may also be prepared by heating chlorophenylacetic acid ethyl ester with triethyl phosphite to yield α-phosphonophenylacetic acid triethyl ester and hydrolysing this to convert it to the free acid. |
isCitedBy | http://rdf.ncbi.nlm.nih.gov/pubchem/patent/GB-2141124-A |
priorityDate | 1971-02-22-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 46.