| 摘要 |
PROBLEM TO BE SOLVED: To obtain a novel compound which is useful as a therapeutic agent for excitatory amino acid-participating neurological disease and psychiatric disorder. SOLUTION: This novel compound is represented by formula I (R1 -R3 are each H, a halogen, a 1-6C alkyl; R4 is OH, a 1-6C alkyl, amino), typically 7- nitro-2-(1H)-quinoline-3-sulfonic acid. The compound of formula I is prepared by reduction of a compound of formula II with lithium aluminum hydride in a non-protonic solvent to form an alcohol, oxidation of the alcohol with a metal oxide in an inert solvent to an aldehyde of formula III, condensation reaction of the aldehyde with an alkyl malonate of formula IV (alk means a 1-6C alkyl) in a protonic solvent in the presence of an alkali metal alcoholate to give an ester, reaction of the ester with bromine in pyridine to form a compound of formula V, reaction of the compound of formula V with a compound of formula: R'SH (R' is a 1-6C alkyl), followed by oxidation of the product with nitric acid in concentrated sulfuric acid. |
