Institute of Advanced Studies and School of Pharmaceutical and Chemical Engineering, Taizhou University, Taizhou 318000, P. R. China.
School of Pharmaceutical Science, Zhejiang Chinese Medical University, Hangzhou 310053, P. R. China.
J Org Chem. 2021 May 7;86(9):6239-6246. doi: 10.1021/acs.joc.1c00023. Epub 2021 Apr 9.
A convenient one-pot, three-component reaction has been developed for the synthesis of 3-aroylimidazo[1,2-]--heterocycles from aryl ketones and 2-amino--heterocycles using dimethyl sulfoxide as a methylene donor. The reaction proceeds smoothly catalyzed by I in the presence of KSO and affords the desired products in moderate to good yields. This protocol offers significant superiority in accessing biologically active 3-aroylimidazo[1,2-]--heterocycles with various substitution patterns.
一种方便的一锅法、三组分反应已经被开发出来,用于通过使用二甲亚砜作为亚甲基供体,从芳基酮和 2-氨基杂环化合物合成 3-芳酰基咪唑并[1,2-a]-杂环化合物。该反应在 I 的催化下,在 KSO 的存在下顺利进行,以中等至良好的收率得到所需的产物。该方案在获得具有各种取代模式的生物活性 3-芳酰基咪唑并[1,2-a]-杂环化合物方面具有显著的优越性。