期刊
ORGANIC CHEMISTRY FRONTIERS
卷 6, 期 4, 页码 426-431出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c8qo01054d
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资金
- NSFC [21272175]
- fundamental research funds for the central universities
Selective fluorination of 4-substituted 2-aminopyrimidine derivatives with Selectfluor in the presence of Ag2CO3 is presented. The substrates are 4-aryl-or vinyl-or amine-substituted 2-aminopyrimidines. This method gives 4-substituted 5-fluoro-2-aminopyrimidines in fair to high yields with excellent regioselectivities. 5-Fluoro-4-(pyridin-3-yl)-2-aminopyrimidine was transformed into 5-fluoro-N-(2-methyl5- nitrophenyl)-4-(pyridin-3-yl) pyrimidin-2-amine in the synthesis of fluorinated imatinib base.
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