Development of Novel Methodology for the Synthesis of 2, 3-Benzodiazepines and Application for Neuro-therapeutic Agents

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Synthetic and medicinal studies of 2, 3-benzodiazepine derivatives were performed for the purpose of exploring novel drug seeds of neuronal disorders. We could establish new method of constructing 2, 3-benzodiazepine nucleus based on our original tandem electrocyclic reactions using benzocyclobutenes and diazomethylene anion as starting materials, and succeed in constructing a novel diazabenzotropone compounds library. Although these compounds were found not to exhibit neuronal protecting activity, some of them showed notable apoptosis-inducing activity against some lymphoma cells. Thus, we found that novel diazabenzotropone derivatives, synthesized utilizing our original reactions, could be a new candidate of novel anticancer agents.