Shi Taoda, Kaneko Lynn, Sandino Michael, Busse Ryan, Zhang Mae, Mason Damian, Machulis Jason, Ambrose Andrew J, Zhang Donna D, Chapman Eli
College of Pharmacy, Department of Pharmacology and Toxicology, the University of Arizona, 1703 E. Mabel St., PO Box 210207, Tucson, Arizona 85721.
ACS Sustain Chem Eng. 2019 Jan 7;7(1):1524-1528. doi: 10.1021/acssuschemeng.8b05276. Epub 2018 Dec 14.
Thieno[2,3-]pyrimidin-4(3)-ones are important pharmacophores that previously required a three step synthesis with two chromatography steps. We herein report a green approach to the synthesis of this pharmacologically important class of compounds via a catalytic four-component reaction using a ketone, ethyl cyanoacetate, S and formamide. The reported reaction is characterized by step economy, reduced catalyst loading and easy purification.
噻吩并[2,3 - ]嘧啶 - 4(3) - 酮是重要的药效基团，此前需要三步合成且包含两步色谱分离步骤。我们在此报告了一种绿色合成方法，通过使用酮、氰基乙酸乙酯、硫和甲酰胺进行催化四组分反应来合成这类具有重要药理作用的化合物。所报道的反应具有步骤经济性、降低催化剂用量以及易于纯化的特点。
