Unusual synthesis of new glycine antagonists via sequential aldol condensation-lactonization-elimination reaction

Compounds 2 and 3 were designed in order to probe the North-East region of the strichnine-insensitive glycine binding site of the NMDA receptor. The two products were obtained readily by a tandem aldol condensation-lactonization-elimination step which affords the desired isomer with complete regioselection.