2-[(4-nitrophenyl)amino]ethanol is used to prepare phenylpurinediamine derivatives as a class of reversible kinase inhibitors targeting both EGFR-activating and resistance mutations of lung cancer. It is also used to synthesize benzannulated N-heterocycles via palladium-catalyzed domino intermolecular alkylation/intramolecular amination of functionalized aryl iodides and bromoalkylamines.