Ag 促进的未保护的 4,6-二取代 2-氨基嘧啶与 Selectfluor 的氟化反应。
Ag-Assisted Fluorination of Unprotected 4,6-Disubstituted 2-Aminopyrimidines with Selectfluor.
机构信息
Shanghai Key Lab of Chemical Assessment and Sustainability, School of Chemical Technology and Engineering, Tongji University , 1239 Siping Road, Shanghai 200092, People's Republic of China.
出版信息
J Org Chem. 2017 Jan 20;82(2):1260-1265. doi: 10.1021/acs.joc.6b02624. Epub 2017 Jan 6.
A direct fluorination of 4,6-disubstituted 2-aminopyrimidines with Selectfluor in the presence of Ag(I) is presented, affording the corresponding 4,6-disubstituted 5-fluoro-2-aminopyrimidines with acceptable to high yield. Ag(I) is crucial for this chemoselective fluorination process. The transformation of 4,6-diphenyl 5-fluoro-2-aminopyrimidine into N-(5-fluoro-4,6-diphenylpyrimidin-2-yl)-4-methylbenzenesulfonamide is discussed, and the reaction mechanism is investigated, as well.
本文介绍了在 Ag(I) 存在下，用 Selectfluor 对 4,6-二取代 2-氨基嘧啶进行直接氟化反应，以中等到高产率得到相应的 4,6-二取代 5-氟-2-氨基嘧啶。Ag(I) 对该选择性氟代反应过程至关重要。讨论了 4,6-二苯基 5-氟-2-氨基嘧啶转化为 N-(5-氟-4,6-二苯基嘧啶-2-基)-4-甲基苯磺酰胺的反应，并对反应机理进行了研究。
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