Study of Environmentally Benign One-Pot Syntheses of Heterocyclic Key Intermediates for Drug

以苯乙烯为原料，研究了咪唑、噻唑和恶唑的一锅合成工艺；然而，我们无法得到相应的杂环化合物。由于在反应混合物中检测到相当数量的中间体phenacyl halides，偶联试剂（例如硫酰胺）的失活被认为是产生这些结果的原因。我们认为，进一步优化偶联剂活化的反应条件，可以实现这些杂环化合物的一锅合成。

We studied one-pot syntheses of imidazoles, thiazoles and oxazoles from styrenes; however, we could not obtain the corresponding heterocyclic compounds. Since considerable quantity of intermediates phenacyl halides were detected in the reaction mixture, deactivation of coupling reagents, for example thioamides, is thought to be the reason for these results. We believe that further optimization of reaction conditions for activation of coupling reagent develops one-pot synthesis of these heterocyclic compounds.