Process for the manufacture of quinoline derivatives
First Claim
1. A process for the preparation of the compounds of general formula (I) whereinR 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”
;
in a solvent selected from straight or branched alkanes and cycloalkanes or mixtures thereof with a boiling point between 80 and 200°
C.
1 Assignment
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Accused Products
Abstract
A process for the preparation of the compounds of general formula (I)
wherein R is selected from methyl, ethyl, n-propyl, iso-propyl, n-butyl, iso-butyl, sec.-butyl and allyl; R5 is selected from the 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 form hydrogen, fluoro and chloro, with the proviso that R″ is selected from fluoro and chloro only when R′ is selected from fluoro and chloro; by reacting a quinoline-3-carboxylic acid ester derivative of formula A with an aniline derivative of formula B
in a solvent selected from straight or branched alkanes and cycloalkanes or mixtures thereof with a boiling point between 80 and 200° C.
-
Citations
6 Claims
-
1. A process for the preparation of the compounds of general formula (I)
wherein R 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;
orR5 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”
;
in a solvent selected from straight or branched alkanes and cycloalkanes or mixtures thereof with a boiling point between 80 and 200°
C.- View Dependent Claims (2, 3, 4, 5, 6)
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Specification