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Rh- and Cu-Cocatalyzed Aerobic Oxidative Approach to Quinazolines via [4 + 2] C-H Annulation with Alkyl Azides

Xiaoyang Wang and Ning Jiao*

*State Key Laboratory of Natural and Biomimetic Drugs, Peking University, Xue Yuan Road 38, Beijing 100191, China, Email:

X. Wang, N. Jiao, Org. Lett., 2016, 18, 2150-2153.

DOI: 10.1021/acs.orglett.6b00774 (free Supporting Information)

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An efficient rhodium- and copper-co-catalyzed C-H bond activation and [4 + 2] annulation enables the construction of bioactively important quinazolines. This aerobic oxidative protocol provides a useful application of simple azides in N-heterocycle synthesis with N2 and H2O as byproducts.

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proposed mechanism

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ID: J54-Y2016