摘要
As important constitutes in many drugs, piperazine comprised compounds are of great interest for drug design. In this paper, two piperazine-based compounds were synthesized for the first time, with different strategies exploited. For one compound, a highly reactive intermediate of isothiocyanate was constructed to get the desired piperazinecarbothioamide. The synthesis of the other compound was completed sequentially through Friedel-Crafts acylation, coupling reaction and Michael addition. Both synthetic routes have short steps and acceptable yields, and such strategies can be applied to the synthesis of similar oioerazine-containin~ comoounds.
哌嗪环是许多上市药物结构中的重要组成部分,在药物设计中有重要作用。本文首次以不同策略合成了两个含哌嗪的化合物。对于其中一个目标物,通过具有高反应活性的异硫氰酸酯中间体来构建哌嗪硫代酰胺结构。另一目标化合物通过傅克酰化、偶联反应和麦克加成构建。两条合成路线均有步骤短、产率高的优点,可为类似含哌嗪化合物的合成提供参考。
基金
National Basic Research Program of China(Grant No.2012CB518000)
the National Natural Science Foundation of China(Grant No.21172012)
the Specialized Research Fund for the Doctoral Program of Higher Education of China(Grant No.20120001110010)
