School of Chemistry and Chemical Engineering, Nanchang University, 999 XueFu Road, Nanchang, 330031, China.
Org Biomol Chem. 2023 Mar 8;21(10):2069-2080. doi: 10.1039/d3ob00087g.
A formal [3 + 2] annulation reaction of crotonate-derived sulfur ylides and β-ketothioamides (KTAs) was successfully developed to produce good-to-excellent yields of thiazoline and spiro[indoline-3,3'-thiophene] scaffolds. This transformation is a powerful tool for the synthesis of thiazoline and spiro[indoline-3,3'-thiophene] scaffolds due to its mild reaction conditions, easily accessible starting materials, and broad substrate scope. A large-scale reaction was carried out to ensure the practical applicability of this methodology. Finally, the plausible mechanistic pathway of the developed methodology was investigated.
成功开发了一种基于巴豆酸盐衍生的硫叶立德和β-酮硫代酰胺（KTAs）的[3+2]环加成反应，以高产率合成了噻唑啉和螺[吲哚啉-3,3'-噻吩]骨架。由于其温和的反应条件、易得的起始原料和广泛的底物范围，这种转化是合成噻唑啉和螺[吲哚啉-3,3'-噻吩]骨架的有力工具。进行了大规模反应以确保该方法的实际适用性。最后，研究了所开发方法的合理的机理途径。
