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This book describes the incorporation of 2-[4'-oxadiazolo, imidazo, benzimidazo, thiadiazolo, isoxazolo, and pyrazolo] derivatives on to the 1,4-benzodiazepine nucleus through phenoxyl/ phenylamino spacer from the corresponding amidine, imidate ester, thiosemicarazone, dimethylaminomethylene ketone, and chalcone derivatives. The structures of all compounds have been established by elemental analysis, IR, 1H NMR, 13C NMR, and MS spectral data.