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 Oct 1;86(19):13734-13743. doi: 10.1021/acs.joc.1c01847. Epub 2021 Sep 20.
An efficient, facile, and eco-friendly synthesis of pyrimidine derivatives has been developed. It involves a [3 + 2 + 1] three-component annulation of amidines, ketones, and one carbon source. ,-Dimethylaminoethanol is oxidized through C(sp)-H activation to provide the carbon donor. One C-C and two C-N bonds are formed during the oxidative annulation process. The reaction shows good tolerance to many important functional groups in air, making this methodology a highly versatile alternative, and significant improvement to the existing methods for structuring a pyrimidine framework, especially 4-aliphatic pyrimidines.
一种高效、简便、环保的嘧啶衍生物合成方法已经被开发出来。它涉及到酰胺、酮和一个碳源的[3 + 2 + 1]三组分环化反应。通过 C(sp)-H 活化氧化 -二甲氨基乙醇提供碳供体。在氧化环化过程中形成一个 C-C 键和两个 C-N 键。该反应对空气中许多重要官能团具有良好的耐受性，使这种方法成为一种高度通用的替代方法，对现有的构建嘧啶骨架的方法，特别是 4-脂肪族嘧啶，有显著的改进。
