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Selective addition of amines to 5-trifluoromethyl-2, 4-dichloropyrimidine induced by Lewis acids

DT Richter, JC Kath, MJ Luzzio, N Keene, MA Berliner…

文献索引:Richter, Daniel T.; Kath, John C.; Luzzio, Michael J.; Keene, Nandell; Berliner, Martin A.; Wessel, Matthew D. Tetrahedron Letters, 2013 , vol. 54, # 35 p. 4610 - 4612

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被引用次数: 4

摘要

Abstract A variety of 2, 4-diamino-pyrimidine systems can be prepared from the corresponding 2, 4-dichloro-pyrimidine by sequential addition of two amines, the first adding selectively to the 4-position. In contrast it was found that 2, 4-dichloro-5-trifluoromethyl- pyrimidine yields a 1: 1 mixture of the two possible isomers. Lewis acids were employed to increase the ratio of isomers to> 10: 1 in favor of the 2-addition product. Optimization of the ...