Abstract A tandem reduction-reductive amination reaction has been applied to the synthesis of (±)-4-alkyl-2, 3, 4, 5-tetrahydro-1, 5-benzoxazepines and (±)-4-alkyl-1-benzoyl-2, 3, 4, 5- tetrahydro-1H-1, 5-benzodiazepines. The nitro aldehydes and ketones required for 1, 5- benzoxazepine ring closures were prepared by nucleophilic aromatic substitution of the alkoxides from several 3-buten-1-ol derivatives with 2-fluoro-1-nitrobenzene followed by ...