ABSTRACT
An Rh(III)-catalyzed synthesis of unsymmetrical acridines from aldehydes and azides through bilateral cyclization process in biomass-derived γ-valerolactone has been developed. The in situ-generated imino directing group (DG) from aldehyde and catalytic amount of BnNH2 worked as a transient directing group, thereby no additional steps were required for installation and removal of the DG. A series of functional groups were well tolerated, affording the desired products in good to excellent yields. Gram-scale synthesis of the product was also achieved.