Gao Ming-Yuan, Li Jing-Hang, Zhang Shi-Bo, Chen Li-Jun, Li Yue-Sheng, Dong Zhi-Bing
School of Chemistry and Environmental Engineering , Wuhan Institute of Technology , Wuhan 430205 , China.
Hubei Key Laboratory of Radiation Chemistry and Functional Materials, School of Nuclear Technology and Chemistry & Biology , Hubei University of Science and Technology , Xianning 437100 , China.
J Org Chem. 2020 Jan 17;85(2):493-500. doi: 10.1021/acs.joc.9b02543. Epub 2019 Dec 31.
A highly efficient synthetic method for the preparation of 2-aminobenzothiazoles starting from arylthioureas has been reported. By using a nickel catalyst, arylthioureas undergo intramolecular oxidative C-H bond functionalization, giving the desired 2-aminobenzothiazoles in good to excellent yields. This protocol features an inexpensive catalyst, low catalyst loading, mild reaction conditions, a short reaction time, and good to excellent yields, and it can be scaled up easily to a gram scale with almost no yields decreasing.
据报道，一种从芳基硫脲出发制备2-氨基苯并噻唑的高效合成方法。通过使用镍催化剂，芳基硫脲发生分子内氧化C-H键官能化反应，以良好至优异的产率得到所需的2-氨基苯并噻唑。该方法具有催化剂廉价、催化剂用量低、反应条件温和、反应时间短、产率良好至优异等特点，并且可以很容易地扩大到克级规模，几乎不降低产率。
