The Chan–Evans–Lam reaction of 1-unsubstituted 4-fluoroalkylpyrimidin-2(1Н)-ones with arylboronic acids is reported as a facile synthetic route to hitherto unavailable N1-(het)aryl and N1-alkenyl derivatives of the corresponding pyrimidines. An efficient C–N bond-forming process is also observed by using boronic acid pinacol esters as coupling partners in the presence of Cu(II) acetate and boric acid. The 4-fluoroalkyl group on the pyrimidine ring significantly assists in the formation of the target N1-substituted products, in contrast to the 4-methyl and 4-unsubstituted substrates which do not undergo N1-arylation under similar reaction conditions.

中文翻译：

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Chan-Evans-Lam 4-氟烷基嘧啶-2（1H）-一个的N1-（杂）芳基化和N1-烯基化

的赞埃文斯-Lam反应1-未取代-4- fluoroalkylpyrimidin-2（1 Н） -酮与芳基硼酸报告为简便的合成路线，以迄今不可用Ñ 1-（杂）芳基和Ñ的1-烯衍生物相应的嘧啶。在乙酸铜（II）和硼酸的存在下，通过使用硼酸频哪醇酯作为偶联伙伴，也观察到了有效的C–N键形成过程。与在相似的反应条件下不进行N 1-芳基化的4-甲基和4-未取代的底物相反，嘧啶环上的4-氟烷基大大地帮助了目标N 1-取代的产物的形成。