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通过 5-烯丙氧基取代恶唑的 [4 + 2]-环加成反应合成稠合二氢吡喃(呋喃)吡啶。

Synthesis of fused dihydropyrano(furano)pyridines via [4 + 2]-cycloaddition of 5-alkenoxy substituted oxazoles.

机构信息

Chemical Development-Synthetic Chemistry, GlaxoSmithKline R&D, 709 Swedeland Road, King of Prussia, Pennsylvania 19406, United States.

出版信息

Org Lett. 2012 Mar 16;14(6):1604-7. doi: 10.1021/ol300351v. Epub 2012 Mar 7.

Abstract

A three-step procedure to access fused pyridines has been developed utilizing inexpensive amino acids and alkenols to form the key oxazole precursors. Yields are good to excellent and provide a rapid and inexpensive route to a range of pharmacologically and biologically valuable fused pyridines with difficult to access substitution patterns.

摘要

已开发出一种三步法来获得融合吡啶,该方法利用廉价的氨基酸和烯醇来形成关键的恶唑前体。产率良好到优秀,并为一系列具有难以获得的取代模式的具有药理和生物学价值的融合吡啶提供了快速且廉价的途径。

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