4.7 Article

Sulfone-Mediated SNAr Reaction as a Powerful Tool for the Synthesis of 4-Quinolinyl Ethers and More-Application to the Synthesis of HCV NS3/4a Protease Inhibitor BI 201420

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JOURNAL OF ORGANIC CHEMISTRY
卷 85, 期 13, 页码 8339-8351

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AMER CHEMICAL SOC
DOI: 10.1021/acs.joc.0c00554

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An efficient general methodology for the synthesis of 4-quinolinyl ethers is demonstrated via a highly reactive SNAr reaction of 4-quinolinyl sulfones with a range of structurally diversified 1 degrees, 2 degrees, and 3 degrees alcohols with a wide substrate scope and high yields. By adapting this methodology, a convergent synthesis of a complex target of HCV NS3/4a protease inhibitor BI 201420 was accomplished.

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