4.8 Article

Ruthenium-Catalyzed Straightforward Synthesis of 1,2,3,4-Tetrahydronaphthyridines via Selective Transfer Hydrogenation of Pyridyl Ring with Alcohols

期刊

ORGANIC LETTERS
卷 17, 期 16, 页码 4054-4057

出版社

AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.5b01976

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资金

  1. National Natural Science Foundation of China [21472052]
  2. Science Foundation for Distinguished Young Scholars of Guangdong Province [2014A030306018]
  3. Fundamental Research Funds for the Central Universities [2014ZZ0047, 2015PT018]

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Through a ruthenium-catalyzed selective hydrogen transfer coupling reaction, a novel straightforward synthesis of 1,2,3,4-tetrahydronaphthyridines from o-amino-pyridyl methanols and alcohols has been developed. The synthetic protocol proceeds in an atom- and step-economic fashion together with the advantages of operational simplicity, broad substrate scope, production of water as the only byproduct, and no need for external reducing reagents such as high pressure H-2 gas, offering a highly practical approach for accessing this type of structurally unique products.

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