The purpose of the current study was to construct a β-cyclodextrin drug carrier for rubropunctatin to improve its water solubility and light stability for future cytotoxicity studies.

Herein, we report a nickel-catalyzed oxidative coupling reaction for the synthesis of 3-azo-substituted 2oxindoles. The key intermediates of 3-arylazohexahydropyrrolo-[2,3-b]indoles undergo further transformation to provide 3-azo-substituted 2-oxindoles in the presence of H 2 O, aryldiazonium tetrafluoroborate salts and catalytic amount of NiBr 2 . This reaction can be performed in an open flask at room temperature and exhibits a broad functional-group tolerance in moderate to excellent yields.