Department of Chemistry , Queen's University , 90 Bader Lane , Kingston , Ontario K7L 3N6 , Canada.
Vertex Pharmaceuticals Incorporated, 50 Northern Avenue , Boston , Massachusetts 02210 , United States.
Org Lett. 2018 Jul 6;20(13):3745-3748. doi: 10.1021/acs.orglett.8b01300. Epub 2018 Jun 13.
The Pd-catalyzed regioselective C-H activation/arylation, /iodination, and/acetoxylation reactions of 4-arylpyrimidines using aryl iodides, N-iodosuccinimide, and (diacetoxyiodo)benzene respectively as coupling partners are described. Suzuki-Miyaura coupling and Sonogashira reactions of the resulting aryl iodides are demonstrated. The scalability of the C-H activation/functionalization starting with readily accessible 4-aryl pyrimidines is also reported.
Pd 催化的 4-芳基嘧啶的 C-H 活化/芳基化、碘化和乙酰氧基化反应，分别使用芳基碘化物、N-碘代丁二酰亚胺和（二乙酰氧基碘）苯作为偶联试剂。展示了生成的芳基碘化物的 Suzuki-Miyaura 偶联和 Sonogashira 反应。还报道了以易于获得的 4-芳基嘧啶为起始原料的 C-H 活化/官能化的可扩展性。
