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

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posted on 04.08.2017, 15:43 by Pengfei Shi, Lili Wang, Shan Guo, Kehao Chen, Jie Wang, Jin Zhu
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.