Rhodium-catalyzed C-H activation/annulation of amidines with 4-diazoisochroman-3-imines toward isochromeno[3,4-c]isoquinolines.

A rhodium-catalyzed C-H activation/annulation of amidines with 4-diazoisochroman-3-imines has been established to afford a series of 8-amino-5H-isochromeno[3,4-c]isoquinolines in moderate to good yields with good functional group tolerance. This reaction proceeded in a sequential C-H activation/carbene migration insertion/intramolecular annulation procedure and featured the construction of a C-C and C-N bond in one pot. UV-vis and fluorescence spectral analyses of these highly fused heteroarenes were performed.