Abstract
An efficient method has been developed previously for the synthesis of tetrahydrogenated 1,4-benzodiazepin-5-ones. To extend the reaction application and to study the substituent effect, we used various substituted aryl halides as the starting materials. Substituents on aryl halides including the electron-withdrawing groups such as thio, amino, and trifluoromethyl groups, or the electron-donating group, such as methyl, isopropyl, and phenyl groups have been studied. The desired substituted benzodiazepinones were obtaind in 20–70% yields. We also performed the same reactions with the parent arenes without any substituent and obtained benzodiazepinone in low yield.