http://rdf.ncbi.nlm.nih.gov/pubchem/patent/PL-86959-B1

Outgoing Links

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classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D499-00
classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D501-10
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D499-32
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D499-04
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filingDate 1972-06-12-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 1976-06-30-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber PL-86959-B1
titleOfInvention 7-methoxycephalosporin derivatives[gb1377704a]
abstract 1377704 6-Methoxy penicillins and 7- methoxy cephalosporins MERCK & CO Inc 13 June 1972 [18 June 1971 13 Dec 1971] 27622/72 Heading C2C The invention comprises penicillins of the Formula V and esters thereof in which Š is an acetoxy, hydroxy or carbamoyloxy radical, m is 0 or 1 and R is the grouping where R<SP>2</SP> is a hydrogen or fluorine atom or an amino, guanidino, hydroxy, carboxy, tetrazolyl, sulpho or sulphamino radical and R<SP>3</SP> is a substituted or unsubstituted phenyl, phenoxy or phenylthio radical or a monocyclic 5- or 6- membered heterocyclic ring containing 1 to 4 hetero atoms selected from oxygen, sulphur and nitrogen. The invention also comprises cephalosporins of the Formula VI or esters thereof, in which A<SP>11</SP> is a hydrogen atom or a hydroxy, acetoxy or carbamoyloxy radical, R is as defined above and R<SP>11</SP> is a hydrogen atom or an acyl radical. The invention further comprises a process that comprises treating a compound of Formula VII in which A is a hydrogen atom or an acetoxy or carbamoyloxy radical, R is an acyl radical and R<SP>1</SP> is a blocking group, with an acid at an elevated temperature to produce a compound of the Formula I wherein A, R and R<SP>1</SP> are as defined above. The reaction may be conducted under anhydrous conditions in the presence of a drying agent. The acid may be a phosphoric acid, sulphuric acid, sulphonic acid, phosphonic acid, trifluoroacetic acid, dihalomethylphosphonic acid, a monoalkyl ester of sulphuric acid or a monoester of phosphoric acid. In the above-described process for preparing a compound of Formula I, the use of some of the acid catalysts, such as sulphuric acid and the sulphate esters, may also result in the formation of a by-product of Formula VIII wherein A, R and R<SP>1</SP> are as defined above. However, by-product VIII may be converted to compound I by heating it with an acid anhy. dride in the presence of a tertiary amide solvent.n[GB1377704A]
priorityDate 1971-06-18-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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