Department of Chemistry, Fuzhou University , Fuzhou 350108, China.
Org Lett. 2014 Jun 20;16(12):3284-7. doi: 10.1021/ol501290p. Epub 2014 Jun 4.
The CF3S-substituted moiety serves as an important structural element in many bioactive molecules. A versatile copper catalyst that allowed for trifluoromethylthiolation of primary and secondary α-bromoketones is described. The reaction with readily available elemental sulfur and CF3SiMe3 afforded a broad scope and moderate to good yields of α-trifluoromethylthio-substituted ketones. This procedure represents a very operationally simple yet powerful strategy for the synthesis of α-trifluoromethylthio-substituted ketones, a useful and versatile class of synthetic synthons.
CF3S 取代基在许多生物活性分子中是一个重要的结构单元。本文描述了一种多功能的铜催化剂，它可以实现伯溴代酮和仲溴代酮的三氟甲基硫代化反应。该反应使用易得的元素硫和 CF3SiMe3，具有广泛的底物范围和中等至良好的α-三氟甲基硫代取代酮收率。该方法代表了一种非常操作简单但强大的α-三氟甲基硫代取代酮合成策略，是一类有用且多功能的合成前体。
