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    Copper-Catalyzed Oxidative Amination of Benzoxazoles via C−H and C−N Bond Activation: A New Strategy for Using Tertiary Amines as Nitrogen Group Sources
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    Abstract:
    An efficient and conceptually new method for oxidative amination of azoles with tertiary amines via copper-catalyzed C-H and C-N bond activation has been developed. This protocol can be performed in the absence of external base and only requires atmospheric oxygen as oxidant. The catalyst system is very simple and efficient, which opens a new way for using tertiary amines as nitrogen group sources for C-N bond formation reactions.
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    Functional group
    Abstract A novel and efficient Rh‐catalyzed intermolecular C–H amination of heteroarylarenes with aryl azides has been developed. This procedure does not require an oxidant, releases N 2 as the only byproduct, and provides an efficient approach to diarylamines with broad functional‐group tolerance.
    Functional group
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    Abstract Introducing the primary amino group into aromatic ring is one of the most important study issues in organic chemistry, particularly for the pharmaceuticals and agrochemicals chemistry. Herein, we describe a photoinduced direct C−H amination of arenes with ammonia via the site‐selective C−H thianthrenation that forms a new C−N bond with excellent regioselectivity. The reaction is carried out under mild conditions, and with a wide range of functional group tolerance, such as sensitive −Cl, −Br, and −OH groups which are poorly tolerated in conventional approaches. Moreover, the synthetic utility of our amination protocol has been confirmed through late‐stage modification and gram‐scale synthesis of complex drug‐like molecules.
    Functional group
    Primary (astronomy)
    Organic Synthesis
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    Functional group
    Cleavage (geology)
    Bond cleavage
    Citations (98)
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    Nitrogen atom
    Functional group
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    Chemoselectivity
    Functional group
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    Atom economy
    Functional group
    Nitrogen atom
    Reaction conditions
    Alkyne
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    Transient (computer programming)
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    Functional group
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    Functional group
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    Functional group
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