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Process for the manufacture of quinoline derivatives

  • US 6,875,869 B2
  • Filed: 06/12/2003
  • Issued: 04/05/2005
  • Est. Priority Date: 06/12/2002
  • Status: Active Grant
First Claim
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1. A process for the preparation of the compounds of general formula (I) embedded imagewhereinR is selected from methyl, ethyl, n-propyl, iso-propyl, n-butyl, iso-butyl, sec.-butyl and allyl;

  • R5 is selected from methyl, ethyl, n-propyl, iso-propyl, methoxy, ethoxy, methylthio, ethylthio, n-propylthio, methylsulphinyl, ethylsulphinyl, fluoro, chloro, bromo, trifluoromethyl, and OCHxFy;

    wherein x=0-2, y=1-3 with the proviso that x+y=3;

    R6 is hydrogen;

    or R5 and R6 taken together are methylenedioxy;

    R′

    is selected from methyl, methoxy, fluoro, chloro, bromo, trifluoromethyl, and OCHxFy, wherein x=0-2, y=1-3 with the proviso that x+y=3;

    R″

    is selected from hydrogen,fluoro and chloro, with the proviso that R″

    is selected from flouro and chloro only when R′

    is selected from flouro and chloro;

    by reacting a quinoline-3-carboxylic acid ester derivative of formula A with an aniline derivative of formula B according to the following reaction diagram, to give the compound of general formula (I), designated “

    C”

    , and methanol, designated “

    D”

    ;

    embedded imagein a solvent selected from straight or branched alkanes and cycloalkanes or mixtures thereof with a boiling point between 80 and 200°

    C.

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