http://rdf.ncbi.nlm.nih.gov/pubchem/patent/GB-1240687-A
Outgoing Links
Predicate | Object |
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assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_97a285d8ecd0184a7e5d89a1e4e07997 |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C12P41-007 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D501-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D501-20 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C12P41-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D501-32 |
filingDate | 1968-09-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_a24f50e4d2536a30521e2d25edc6d31c |
publicationDate | 1971-07-28-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | GB-1240687-A |
titleOfInvention | Antibacterial agents and a process for the preparation thereof |
abstract | 1,240,687. Cephalosporin compounds; pharmaceutical compositions; glycines. BRISTOLMYERS CO. 5 Sept., 1968 [5 Sept., 1967 (3)], No. 42345/68. Headings C2A and C2C. Novel cephalosporin compounds of the general formula and wherein R<SP>1</SP> is H or acetoxy and R<SP>2</SP> and R<SP>3</SP> are H or Cl, and the non-toxic, pharmaceutically acceptable salts thereof are prepared, in the case of compounds of Formula I, by acylating a compound of the general formula or a carboxylic acid salt thereof with an acid of the formula or an acylating derivative or mixed anhydride thereof, wherein -NXY is a protected amino group in which X is H and Y is t-butoxycarbonyl, benzyloxycarbonyl or 2,2,2-trichloroethoxy carbonyl or like protecting group or X and Y taken together represent a 2-hydroxy-lnaphthylmethylene group or a like protecting group in an inert solvent at a temperature below 0 C. and subsequently removing the protecting group; and then optionally forming a salt or reacting with acetone at a temperature of - 20 to 50 C. to give a compound of Formula II. The acylating acids of general Formula IV are prepared from the corresponding unprotected amines by known methods. The D-(-)-2- (p-hydroxyphenyl) glycine is prepared by the following series of reactions: (A) p-anisaldehyde + NaCN+NH 4 OH (E) The product of reaction (D) is heated with 48% HBr to yield the corresponding hydroxy compound. D - ( - ) - α - (p - hydroxyphenyl) - α - (t - butoxycarbonylamino) acetic acid is prepared by reacting a suspension of D-( - )-2-(p-hydroxyphenyl)- glycine and magnesium oxide, in dioxane-water, with t-butoxycarbonyl azide. The corresponding 3-chloro- and 3,5-dichloro-compounds are similarly prepared by using the appropriate chloro-substituted glycines as starting materials. The 3 - chloro- and 3,5 - dichloro - derivatives of D - ( - ) - 2 - (p - hydroxyphenyl) glycine are prepared by treating the hydrochloride of the glycine with one or two moles, respectively, of sulfuryl chloride in glacial acetic acid. D - ( - ) - α - carbobenzoxyamino - α - (4 - carbohenzoxyoxyphenyl) acetic acid is prepared by reacting D-( - )-2-(p-hydroxyphenyl) glycine with carbobenzoxychloride. Pharmaceutical compositions comprise a compound of Formula I or II and a carrier or diluent. The compositions, or active ingredients thereof, may be used to treat animals, including poultry. |
isCitedBy | http://rdf.ncbi.nlm.nih.gov/pubchem/patent/DE-2422385-A1 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/JP-S57185291-A http://rdf.ncbi.nlm.nih.gov/pubchem/patent/JP-S49135989-A http://rdf.ncbi.nlm.nih.gov/pubchem/patent/JP-S4985002-A http://rdf.ncbi.nlm.nih.gov/pubchem/patent/JP-S5036485-A http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-4160863-A http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-4234721-A http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-RE31730-E http://rdf.ncbi.nlm.nih.gov/pubchem/patent/JP-S6043073-B2 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-4504657-A http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-5003064-A |
priorityDate | 1967-09-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 53.