Chemical Development US, Boehringer-Ingelheim Pharmaceuticals Inc., 900 Ridgebury Road, P.O. Box 368, Ridgefield, Connecticut 06877-0368, United States.
Material and Analytical Sciences US, Boehringer-Ingelheim Pharmaceuticals Inc., 900 Ridgebury Road, P.O. Box 368, Ridgefield, Connecticut 06877-0368, United States.
J Org Chem. 2020 Jul 2;85(13):8339-8351. doi: 10.1021/acs.joc.0c00554. Epub 2020 Jun 19.
An efficient general methodology for the synthesis of 4-quinolinyl ethers is demonstrated via a highly reactive SAr reaction of 4-quinolinyl sulfones with a range of structurally diversified 1°, 2°, and 3° 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 was accomplished.
本文展示了一种高效的 4-喹啉基醚合成通用方法,即通过 4-喹啉基砜与一系列结构多样的 1°、2°和 3°醇的高反应性 SAr 反应进行合成,具有广泛的底物范围和高收率。通过采用这种方法,完成了 HCV NS3/4a 蛋白酶抑制剂复杂目标物的收敛合成。