Department of Chemistry, Masaryk university, Kotlářská 2, Brno 611 37, Czech Republic.
Molecules. 2020 May 6;25(9):2168. doi: 10.3390/molecules25092168.
We reported a novel simplified synthetic procedure for the preparation of monosubstituted piperazine derivatives which can now be easily prepared in a one-pot-one-step way from a protonated piperazine with no need of introduction of a protecting group. Reactions, proceeding either at room or higher temperatures in common solvents, involve heterogeneous catalysis by metal ions supported on commercial polymeric resins. A general synthetic scheme was successfully applied to afford a wide range of monosubstituted piperazines. Furthermore, we picked up a set of piperazine derivatives and studied the possibilities of microwave acceleration of given synthetic reactions to make them even more efficient. Our research proceeded from a simple batch technique to the construction of a flow microwave reactor prototype and resulted in promising findings which are summarized and discussed in the article.
我们报道了一种新颖的简化合成程序，用于制备单取代哌嗪衍生物，现在可以从质子化的哌嗪中很容易地以一锅一步的方式制备，而无需引入保护基团。反应在室温或更高温度下在常见溶剂中进行，涉及商业聚合物树脂负载的金属离子的多相催化。一个通用的合成方案被成功地应用于提供广泛的单取代哌嗪。此外，我们选择了一组哌嗪衍生物，并研究了微波加速给定合成反应的可能性，以使它们更加高效。我们的研究从简单的分批技术发展到构建流微波反应器原型，并取得了有希望的发现，这些发现总结并在文章中进行了讨论。
