SYNTHESIS OF PYRIDO 1,2-a PYRIMIDINONE SERIES OF COMPOUMDS, POTENTIAL AGENTS ON THE NERVOUS SYSTEM

In an effort to modify the structure of edulinine so to seek compounds exhibiting higher potency toward inhibition of central nervous system, we designed and synthesized several analogous compounds: 2-methoxy-3-(3-methyl-2-butenyl)-4-oxo-4 H-pyrido 1, 2-a pyrimidine (Ⅳ), 4-methoxy-3-(3-methyl-2-butenyl)-2-oxo-2H-pyrido1, 2-apyrimidine (Ⅴ), 2-methoxy-3-(2, 3-dihydroxy-3-methyl-1-butyl)-4-oxo-4H-pyrido1,2-a pyrimidine (Ⅵ), and 4-methoxy-3-(2,3-dihydroxy-3-methyl-1-butyl)-2-oxo-2H-pyrido1,2-apyrimidine(Ⅶ). Animal experiments revealed that compound (Ⅳ) has anticonvulsant activity, compounds (Ⅴ) and (Ⅵ) have far lower activity than compound (Ⅳ).