3-(1,2,4-OXADIAZOLYL)-5,6,7,8-TETRAHYDRO-1,6-NAPHTYRIDINE DERIVATIVE

摘要

PURPOSE:To obtain a new compound having affinity to a benzodiazepine receptor and useful, e.g. as an antianxiety agent, an anticonvulsant and a treating agent for sleep disorder. CONSTITUTION:This compound of formula I [R1 is H, acyl, lower alkyl, R'1CH2- (R'1 is lower cycloalkyl, lower alkenyl, benzyl, aryl, etc.); R2 is lower alkyl, lower cycloalkyl, lower alkenyl, aryl, etc.; R3 and R4 are H or lower alkyl; X is O or S], e.g. 6-benzyl-3-(5-cyclopropyl-1,2,4-oxadiazole-3-yl)-5,6,7,8- tetrahydro-1,6-naphtyridine-2(1H)-one. Further, the compound is obtained, e.g. by the intramolecular cyclodehydration of a compound of formula II (R'2 is same group as R2 with the exclusion of lower alkoxy, lower alkenyloxy, phenoxy and lower alkylthio).