4.8 Article

Cu(I)-Catalyzed Diamination of Disubstituted Terminal Olefins: An Approach to Potent NK1 Antagonist

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ORGANIC LETTERS
卷 11, 期 11, 页码 2365-2368

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AMER CHEMICAL SOC
DOI: 10.1021/ol900808z

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  1. General Medical Sciences of the National Institutes of Health [GM083944-02]

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This paper describes a diamination process using di-tert-butyldiaziridinone as nitrogen source and CuCl as catalyst. A wide variety of disubstituted terminal olefins can be efficiently diaminated in good yields under mild condition. This diamination process was used to synthesize potent NK1 antagonist Sch 425078.

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