| 摘要 |
Method for the preparation of benzo[b]naphthyridines having the general formula (I) wherein the meaning of the substituents is stated in disclosure and consists 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 (V) is effected, and optionally, the ester obtained is transformed into an acid and optionally into a salt. Disclosed are also new benzo[b]naphthyridines prepared by this method.
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