3, 4dihydro-4-oxo-6-quin~~ yl) methyl]-N-prop2-yny~ ino] benzoyl]-~-glutamic acid (1, CB3717) have led to the synthesis of a series of quinoline antifolates bearing a variety of substituents at the C2 and C4 positions. In general the synthetic route involved the coupling of the appropriate diethyl N-[4-(prop2-ynylamino) benzoyl]-~-glutamate with a disubstituted 6- (bromomethy1) quinoline followed by deprotection using mild alkali. The compounds were ...