| 摘要 |
<p>Method for the preparation of benzo[b]naphthyridines having the general formula (I) wherein R is a carboxy, alkyloxycarbonyl, cyano, carbamyl, alkylcarbamyl, benzylcarbamyl, hydroxyethylcarbamyl, dialkylaminoethylcarbamyl or dialkylcarbamyl radical whose alkyl parts may optionally form, with the nitrogen atom to which they are attached, a heterocycle with 5 or 6 members containing optionally another heteroatom selected amongst oxygen, sulphur or nitrogen and optionally substituted on the nitrogen by an alkyl radical, R' is H, alkyl, fluoroalkyl, carboxyalkyl, cycloalkyl (3 to 6C), fluorophenyl, difluorophenyl, alkyloxy or alkylamino, and Hal is halogen, as well as the salts thereof, if any, characterized in that: 1) an amine having the general formula R'-NH-CH2-CH2-R' is condensed, wherein R' is alkyloxycarbonyl, cyano, carbamyl, alkylcarbamyl, benzylcarbamyl, hydroxyethylcarbamyle, dialkylaminoethylcarbamyl or dialkylcarbamyl whose alkyl parts may optionally form, with the nitrogen atom to which they are attached, a heterocycle with 5 or 6 members containing optionally another heteroatom selected amongst oxygen, sulphur or nitrogen and optionally substituted on the nitrogen by an alkyl radical, on a chloro fluoro quinoline having the general formula (II) wherein R1 is an alkyl radical, the alkyl radicals mentioned hereabove having from 1 to 4C and being straight or branched; 2) a cyclisation of the fluoroquinoline of general formula (III) is effected, wherein R1 is defined as hereabove in 1); 3) an oxidation of tetrahydro-1,2,3,4 benzo[b]naphthyridine-1, 8 having a general formula (IV) is effected, and optionally, the ester obtained is transformed into an acid and optionally into a salt.</p> |
