A facile one-pot synthesis of trifluoromethylated pyrimidines has been achieved by the treatment of fluorinated 2-bromoenones with aryl- and alkylamidines. The assembly of pyrimidine core proceeds by the cascade reactions via aza-Michael addition–intramolecular cyclization–dehydrohalogenation/dehydration sequence. This strategy is featured by high selectivity and mild reaction conditions giving the target heterocycles in high yields (up to 99%). The unique influence of trifluoromethyl group on the reaction path is demonstrated.

中文翻译：

---

溴烯酮与Am的反应：三氟甲基化嘧啶的无催化剂简单方法

通过用芳基和烷基am处理氟化的2-溴代烯酮，可以轻松地一锅合成三氟甲基化的嘧啶。嘧啶核的组装是通过aza-Michael加成-分子内环化-脱氢卤化/脱水序列的级联反应进行的。该策略的特点是高选择性和温和的反应条件，可高产率（高达99％）提供目标杂环。证明了三氟甲基对反应路径的独特影响。