Highly Efficient One-Pot Synthesis of 2,4-Disubstituted Thiazoles Using Au(I) Catalyzed Oxidation System at Room Temperature
Highly Efficient One-Pot Synthesis of 2,4-Disubstituted Thiazoles Using Au(I) Catalyzed Oxidation System at Room Temperature
复制标题
室温下使用 Au(I) 催化氧化体系高效一锅法合成 2,4-二取代噻唑
作者：
Gongde Wu;Xiaoli Wang;Hao Liu
本文以甲磺酸盐为反离子，成功制备了含莫尔- dalphos配体的金络合催化剂。合成了7种磺酸铵，以促进中间体磺酰氧甲基酮的生产。结果表明，低酸度N，N-二甲基苯甲磺酸盐在该反应中表现出良好的活性。此外，该催化剂有效地避免了由于低酸度而导致的活性损失。将各种硫胺直接加入到反应混合物中，不分离中间产物。然后，在室温下高效合成了20种2,4-二取代噻唑，收率最高达91%。本研究为一锅法合成噻唑及其衍生物提供了一种高效、温和的金催化氧化体系。
In the present work, gold complex catalysts with Mor-DalPhos ligands were successfully prepared using mesylates as counter ions. Seven ammonium sulfonates were synthesized to promote the production of intermediate sulfonyloxymethyl ketone. It was found that low-acidity N,N-dimethylbenzenaminium methanesulfonate showed excellent activity in the reaction. Furthermore, the catalysts effectively avoided the loss of activity due to the low acidity. Various thioamides were directly added to the resulting reaction mixture without the separation of intermediate product. Then, twenty kinds of 2,4-disubstituted thiazoles were efficiently synthesized at room temperature with the highest yield of 91%. This work provides an efficiency and mild gold-catalyzed oxidation system for the one-pot synthesis of thiazole and its derivatives.
影响因子：
16.6
作者：
Ji, Kegong;Zhao, Yulong;Zhang, Liming
通讯作者：
Zhang, Liming