Ag-Assisted Fluorination of Unprotected 4,6-Disubstituted 2-Aminopyrimidines with Selectfluor

详细信息    查看全文

• 作者：Chenxi Wang ; Juewang Cai ; Min Zhang ; Xiaoming Zhao
• 刊名：Journal of Organic Chemistry
• 出版年：2017
• 出版时间：January 20, 2017
• 年：2017
• 卷：82
• 期：2
• 页码：1260-1265
• 全文大小：406K
• ISSN：1520-6904

文摘

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.