Abstract
AbstractA rhodium‐catalyzed cascade cross‐coupling/spirocyclization/formal [4+2] cycloaddition reaction of 3‐(2‐isocyanoethyl)indoles with aromatic azides is developed, providing a general synthetic protocol to polycyclic spiroindolines bearing a pentasubstituted guanidine moiety with moderate to excellent yields. This transformation is highly effective since one C−C, one C=N, three C−N bonds as well as two new rings are constructed in a single step. More importantly, this work represents a new reactivity pattern of 3‐(2‐isocyanoethyl)indole, and thus constitutes an valuable addition to 3‐(2‐isocyanoethyl)indole chemistry.magnified image
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