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A simple palladium-catalyzed one-pot synthesis of 2-substituted 1,5-dihydrobenzo[e][1,2,4]oxadiazepines from corresponding (E)-amidoximes and o-iodobenzyl bromide or 2-bromo-3chloromethylpyridine is described. Of the derivatives prepared 2-[6-(quinolin-2-ylsulfanyl)hexyl]-1,5-dihydrobenzo[e][1,2,4]oxadiazepine exhibits high activity on HT-1080 (hyman fibrosarcoma) and MG-22A (mouse hepatoma) cancer cell lines.

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A new pathway for the preparation of biologically active 2 substituted 1,5-dihydrobenzo[e][1,2,4]oxadiazepines and related compounds by palladium-catalyzed cyclization of amidoximes with o-iodobenzyl bromide or 2-bromo-3-chloromethylpyridine