4.8 Article

Triple-Bond Insertion Triggers Highly Regioselective 1,4-Aminomethylamination of 1,3-Enynes with Aminals Enabled by Pd-Catalyzed C-N Bond Activation

Journal

ORGANIC LETTERS
Volume 21, Issue 2, Pages 535-539

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.8b03847

Keywords

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Funding

  1. National Natural Science Foundation of China [21672199, 21790333, 21702197]
  2. CAS Interdisciplinary Innovation Team
  3. Anhui provincial Natural Science Foundation [1708085MB28]

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A highly chemo- and regioselective 1,4-aminomethylamination of simple enynes with aminals to allenic 1,5-diamines by taking advantage of C-N bond activation has been reported. The reaction proceeds under mild reaction conditions and can be performed under lower catalyst loading (0.1 mol %) with high efficiency and broad substrate scope.

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