A green Passerini three-component reaction of 2-(4-oxo-4,5,6,7-tetrahydro-1H-indol-1-yl)acetic acid with alkyl or aryl isocyanides and aldehydes was reported under aqueous conditions at 35 8C for 1 h, and21 indolone-N-amino acid derivatives were prepared in high yields of [1_TD$IF]42%–99%. Their structures were characterized by IR, ESI–MS, NMR and elemental analysis, and the possible mechanisms have been also proposed. The highly efficient and eco-friendly method provides a facile access to a library of indoloneN-amino acid derivatives for future research on bioactivity screening. A green Passerini three-component reaction of 2- (4-oxo-4,5,6,7-tetrahydro-1H-indol-1-yl) acetic acid with alkyl or aryl isocyanides and aldehydes was reported under aqueous conditions at 35 8C for 1 h, and21 indolone-N-amino acid derivatives were prepared in high yields of [1_TD $ IF] 42% -99%. Their structures were characterized by IR, ESI-MS, NMR and elemental analysis, and the possible mechanisms have The highly efficient and eco-friendly method provides a facile access to a library of indolone N-amino acid derivatives for future research on bioactivity screening.