Rhodium-Catalyzed\nOne-pot Chemoselective Insertion-Rearrangement-Cyclization\nof Azavinyl Carbenes with 2‑Aminobenzyl Alcohols

Chemoselective insertion of in situ generated α-imino\nrhodium\ncarbene onto the O–H bond of 2-aminobenzyl alcohols over the\nN–H bond followed by [1,3]-alky shift has been successfully\naccomplished for the synthesis of amine tethered ketone derivatives.\nThe resultant product was further cyclized under acidic conditions\nto afford biologically important 3-aminoquinolines. Successful integration\nof chemoselective insertion-<i>cum</i>-rearrangement and\ncyclization in one pot offered access to various 3-aminoquinolines\nin a good yield. Conversion of 3-aminoquinolines into biological important\nmotifs has also been demonstrated.