Xia Biao, Chen Wenjun, Zhao Qiongli, Yu Wenquan, Chang Junbiao
College of Chemistry and Molecular Engineering; Collaborative Innovation Center of New Drug Research and Safety Evaluation, Henan Province; School of Pharmaceutical Sciences , Zhengzhou University , Zhengzhou , Henan Province 450001 , China.
Org Lett. 2019 Apr 19;21(8):2583-2587. doi: 10.1021/acs.orglett.9b00541. Epub 2019 Mar 28.
A novel annulation reaction of two enamine molecules with iodine under basic conditions to form 4-functionalized imidazolium salts has been established. In this reaction, iodine acts as both an iodinating reagent and a Lewis acid catalyst. Features of this synthetic method include facilitative preparation of substrates, no use of transition metals, mild reaction conditions, simplicity of operation, and gram scale synthesis.
已建立了一种新颖的反应,即在碱性条件下两个烯胺分子与碘发生环化反应生成4-官能化咪唑鎓盐。在该反应中,碘既作为碘化试剂又作为路易斯酸催化剂。这种合成方法的特点包括底物制备简便、不使用过渡金属、反应条件温和、操作简单以及可进行克级规模合成。