4.8 Article

Base-Promoted N-Pyridylation of Heteroarenes Using N-Propargyl Enaminones as Equivalents of Pyridine Scaffolds

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ORGANIC LETTERS
卷 17, 期 15, 页码 3790-3793

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AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.5b01733

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  1. NSF of China [21202048]
  2. Program for Minjiang Scholar [10BS216]
  3. Xiamen Southern Oceanographic Center [13GYY003NF16]
  4. NSF of Fujian Province, China [2013J01050]
  5. Promotion Program for Young and Middle-aged Teacher in Science and Technology Research of Huaqiao University [ZQN-PY120]

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N-Pyridylation of various N-heteroarenes, including N-heteroarene-containing peptides, was achieved using N-propargyl enaminones (isolated or generated in situ from propargyl amine and propynones) as masked polysubstituted pyridine cores. This metal-free procedure proceeds under mild reaction conditions and generates 1 equiv of H2O as the sole byproduct

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