The synthesis and the NMDA receptor binding affinities of α-amino-3-(phosphonomethyl)-2- naphthalene-propanoic acid, α-amino-3-(phosphonomethyl)-2-benzofuranpropanoic acid, a series of substituted (R)-α-amino-3-(phosphonomethyl)-2-quinolinepropanoic acids,(R)-α- amino-3-(phosphonomethyl)-1, 8-naphthyridine-2-propanoic acid and (R)-α-amino-3- (phosphonomethyl)-1, 6-naphthyridine-2-propanoic acid are reported.