Luo Puying, Ding Qiuping, Ping Yuanyuan, Hu Jianan
Department of Occupational and Environmental Health, School of Public Health, Central South University, 110 Xiang-ya Road, Changsha, Hunan 410078, P. R. China.
College of Chemistry & Chemical Engineering, Jiangxi Normal University, Nanchang, Jiangxi 330022, P. R. China.
Org Biomol Chem. 2016 Mar 14;14(10):2924-9. doi: 10.1039/c6ob00005c.
A mild and efficient tandem benzo[d]thiazole directed C-H iodination and trifluoromethylthiolation for the synthesis of ortho-trifluoromethylthiolated 2-arylbenzo[d]thiazoles have been developed using AgSCF3 as a coupling partner. The reaction exhibits a diverse array of functional group tolerance giving the desired products in good to excellent yields. Regioselective trifluoromethylthiolation was observed at the less sterically hindered site when the phenyl ring of the substrate possesses a methyl group at its meta position.
以AgSCF₃作为偶联伙伴,开发了一种温和高效的串联苯并[d]噻唑导向的C-H碘化和三氟甲硫基化反应,用于合成邻位三氟甲硫基化的2-芳基苯并[d]噻唑。该反应对各种官能团具有良好的耐受性,能以良好至优异的产率得到所需产物。当底物的苯环在其间位具有甲基时,在空间位阻较小的位置观察到区域选择性三氟甲硫基化。