Convenient and practical one-pot synthesis of 4-chloropyrimidines via a novel chloroimidate annulation

…, SM Hoagland, V Rapisardi, S Hollywood…

文献索引：Storz, Thomas; Heid, Richard; Zeldis, Joseph; Hoagland, Steven M.; Rapisardi, Vito; Hollywood, Susan; Morton, George Organic Process Research and Development, 2011 , vol. 15, # 4 p. 918 - 924

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被引用次数: 8

摘要

Reaction of aromatic or heteroaromatic 2-acyl (amino) nitriles with phosphorus pentachloride triggers a novel chloroimidate cyclization, leading directly to the corresponding annullated 4-chloropyrimidines in good to excellent yields. The reaction lends itself to the telescoped one-pot construction of 4-functionalized pyrimidines from the corresponding (hetero) aromatic 2-aminonitriles. For a pyrazolopyrimidine development ...