Formal [4+1] Cycloaddition of o ‐Aminobenzyl Chlorides with Isocyanides: Synthesis of 2‐Amino‐3‐Substituted Indoles

Reaction of substituted o-aminobenzyl chlorides with isocyanides in the presence of a weak base (NaHCO3) at room temperature afforded the diversely functionalized 2-aminoindoles in good to excellent yields. A formal [4+1] cycloaddition of the in situ generated aza-ortho-xylylenes with isocyanides accounted for the reaction outcome.