State Key Laboratory Base of Eco-Chemical Engineering, College of Chemistry and Molecular Engineering, Qingdao University of Science and Technology , Qingdao 266042, P. R. China.
J Org Chem. 2013 Nov 1;78(21):10617-28. doi: 10.1021/jo401397d. Epub 2013 Oct 16.
A rapid and highly efficient method for the regioselective synthesis of thiophene derivatives has been developed by annulation of β-ketothioamides with arylglyoxals and 5,5-dimethyl-1,3-cyclohexanedione in CF3CH2OH within 15 min. The present synthesis has several desirable features, such as high regioselectivity, a concise one-pot protocol, short reaction time, and easy purification. This methodology provides an alternative approach for easy access to tetrasubstituted thiophenes via a one-pot cascade reaction without other additives.
已开发出一种快速高效的方法，通过β-酮硫代酰胺与芳基乙二醛和 5,5-二甲基-1,3-环己二酮在 CF3CH2OH 中于 15 分钟内环合，来实现噻吩衍生物的区域选择性合成。本合成具有几个理想的特点，例如高区域选择性、简洁的一锅法方案、短的反应时间和易于纯化。该方法学提供了一种替代方法，可通过一锅级联反应轻松获得四取代噻吩，而无需其他添加剂。
