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    • 69. 发明专利
    • N-SUBSTITUTED ANTHRANILIC ACIDS
    • GB1391584A
    • 1975-04-23
    • GB2245273
    • 1973-05-10
    • IKEDA MOHANDO CO
    • A61K31/195A61K31/196A61P25/04A61P29/00B01J23/00B01J27/00B01J31/00C07B61/00C07C17/093C07C17/12C07C17/26C07C45/46C07C49/788C07C67/00C07C205/12C07C227/00C07C227/08C07C227/18C07C229/58C07C101/50
    • 1391584 N-naphthyl-anthranilic acids IKEDA MOHANDO CO Ltd 10 May 1973 [11 May 1972] 22452/73 Heading C2C Novel compounds of Formula I in which R 1 is a hydrogen atom, a methyl group or a halogen atom, and R 2 is a halogen atom or an alkyl group containing from 1 to 6 carbon atoms, with the proviso that when R 1 is a hydrogen atom and R 2 is a methyl group, the methyl group R 2 is attached to the 3- or 4- position of the naphthalene nucleus are prepared by reacting together the compounds II and III in which Z is an amino group when Y is a halogen atom and Z is a halogen atom when Y is an amino group, or with a salt of such a naphthylamine or substituted benzoic acid, the reaction being carried out at a temperature of from 80‹ to 230‹ C. and in the presence of a catalyst, whereby the desired acid or salt is obtained, the acid obtained being converted if desired to a salt thereof. Naphthyl intermediates of Formula II above where Z is halogen, are prepared either by halogenation with halogen of the alkyl or dialkyl naphthalene, or by reaction of a halogenation agent, e.g. CuCl 2 , or sodium borofluorate on the diazotized amine of Formula II wherein Y is -NH 2 , the amine being obtained by hydrolysis of the corresponding N-acetyl compound obtained by various means such as halogenation or acylation of a precursor. Pharmaceutical compositions in conventional forms for oral, rectal or topical administration comprise an above novel compound and a carrier or diluent.