PURPOSE: To provide a novel water-soluble, colorless compound useful for treating stroke, epilepsy, schizophrenia or the like, as a strong inhibitor of the pathological phenomena associated with hyperactivation of the excitatory amino acid-dependent pathways of neurotransmission.
CONSTITUTION: A compound represented by formula I, (wherein R1 to R3 are each H, halogen, or the like; and R4 is H, linear or branched 1-6C alkyl, or the like; and R5 is H, hydroxy, or the like), isomers thereof and salts thereof, such as 6,7-dichloro-2(IH)-quinolone-3-phosphonic aicd. The compound is obtained by successively reducing and oxidizing a compound represented by formula II so as to be an aldehyde compound, condensing the same with alkyl malonate, converting the produced compound represented by formula III (wherein alk is linear or branched 1-6C alkyl) into an acid compound followed by reaction with bromine, reacting the product after protection with alkaline metal alkoxide, further reacting the produced compound represented by formula IV (wherein R is alk) with dialkyl phosphite followed by deblocking, and finally treating the same in an acid solvent.
PATORISU DOUSO
JIYAN RUPANIYORU