http://rdf.ncbi.nlm.nih.gov/pubchem/patent/DE-1967024-A1

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assignee http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_05a203d85ee01909eaf728dc16f0f6cb
classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C59-84
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D499-00
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C59-90
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C59-88
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http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D499-00
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C59-90
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C59-84
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C59-88
filingDate 1969-01-03-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_adccf8d19d9fe08cce77bf2f348975ac
publicationDate 1976-06-10-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber DE-1967024-A1
titleOfInvention ACYLPENICILLIN AND METHOD FOR MANUFACTURING THEREOF
abstract (A) Arylcarboxy- and arylcarbothioketene esters of general formulae (I) and (II):- R1 = aryl (thienyl, furyl, pyridyl or phenyl opt. substd. with lower alkyl, Cl, Br, lower alkoxy, di-loweralkylamino or trifluoromethyl) X = halogen (e.g. Cl or Br) X' = X, OR2 or SR7 R2 = phenyl opt. substd. with at least one of: Cl, Br, F, lower alkyl, lower alkoxy, lower alkanoyl, carbo-lower-alkoxy, nitro, di-lower alkylamino, furyl, quinolyl opt. substd. with methyl; phenazinyl, 9,10-anthraquinolyl-, phenanthenequinolyl; anthracenyl, phenanthryl, (1,3-benzodioxolyl), 3-(2-methyl-4-pyronyl), 3-(4-pyronyl) or N-(methylpyridyl), Y2 = -CH=CH-O-, -CH=CH-S-, -CH2-CH2-S-, -CH=N-CH=CH-, -CH=CH-CH=CH-, C(O)-CH=CH.C(O) or -C(O)-C(O)-CH=CH- Z' = -(CH2)3 or -(CH2)4 opt. substd. with methyl, Cl or Br; benzyl opt. substd. with Cl, Br, F, lower alkyl, lower alkoxy, lower alkanoyl, carbo(lower) alkoxy, nitro or di(lower)alkylamino; phthalimidomethyl, benzhydryl, trityl, cholesteryl, alkenyl(max. C8), alkynyl (max.C8), (1-indanyl)methyl, 2-(indanyl) methyl, furylmethyl, pyridylmethyl, (2-pyrrolidino)methyl, (4-imidazolyl)methyl, (2,2-dialkyl-1,3-dioxolon-4-yl)methyl, cycloalkyl and (lower alkyl) substd. cycloalkyl(C3-7), bicyclo(4,4,0)decyl, thujyl, phenchyl, isophenchyl, 7-adamantyl, ac-indanyl opt. substd. with methyl, Br or Cl; ac-tetrahydronaphthyl opt. substd. with methyl, Cl or Br; alkyl or lower alkyl substd. with at least one of Cl, Br, F, nitro, carbo(lower)alkoxy, lower alkanoyl, lower alkoxy, cyano, (lower)alkylmercapto, (lower)alkylsulphinyl, (lower)alkylsulphonyl, -CH2-CH2-NR5R6; -CH2-CH2-CH2-NR5R6; -CH2-CH(CH3)-NR5R6 or -CH(CH3)-CH2-NR5R6, or (lower alkylene)-Y1; NR5R6 = -NH(lower alkanoyl), -N (lower alkyl)2 (where alkyl is same or different), or -N(lower alkyl)anilino Y1 = azetidino, aziridino, pyrrolidino, piperidino, morpholino, thiomorpholino, N-(lower alkyl)-piperazino, pyrrolo, imidazolo, 2-imidazolo, 2,5-dimethylpyrrolidino, 1,4,5,6-tetrahydropyrimidino, 4-methylpiperidino or 2,6-dimethylpiperidino R7 = phenyl opt. mono-, di- or tri-substd. with Cl, Br, F, lower alkyl, lower alkoxy, or trifluoromethyl; only one of the positions in o-pos. to the thio group of the phenyl, is substd. (B) Pharmaceutically acceptable salts of (I) and (II) of general formula (III) R4 = X' = OR2 or SR7 (I) are intermediates for further synthesis. (II) may be used as acylating agents esp. for amines such as 6-APA. (III) are partly known antibacterial agents and may be used in pharmaceutically acceptable antibiotic prepns. which are very effective in the treatment of sensitive Gram-pos. and Gram-neg. infections in man and animals.
priorityDate 1968-01-05-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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