A C–H Activation-Based Strategy for N‑Amino Azaheterocycle Synthesis

A C–H activation-based strategy has been developed for the synthesis of N-amino azaheterocycles. Rh­(III)-catalyzed coupling of N-Boc hydrazones/N-Boc hydrazines with diazodiesters/diazoketoesters provides convenient access to synthetically and medicinally important compounds, N-amino isoquinolin-3-ones and N-amino indoles, by harnessing N-tert-butyloxycarbonyl (N-Boc) cleavage as an adaptable reactivity pattern in distinct synthetic scenarios.