The synthesis of two isomeric dipyrido[1,3]diazepinones (3a,4) and N-monosubstituted derivatives of 3a by cyclocondensation of corresponding bipyridinediamines (1, 2) with urea was described. The alkylation of 3a and 4 with alkyl halides 6 in K2CO3/DMF/TBAB system gave N,N'-disubstituted compounds 7 and 8. Dipyrido[1,3]diazepinones 8a and 3b-d showed a weak general depressive action on the central nervous system and they were also devoid of antidepressant, anxiolytic, anticonvulsant and serotoninolytic or serotoninomimetic properties.
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