Key Laboratory of Small Functional Organic Molecules, Ministry of Education and Jiangxi's Key Laboratory of Green Chemistry , Jiangxi Normal University , Nanchang , Jiangxi 330022 , P. R. China.
Department of Obstetrics and Gynecology , Jiangxi Provincial people's Hospital , Nanchang , Jiangxi 330006 , P. R. China.
J Org Chem. 2019 Oct 18;84(20):12784-12791. doi: 10.1021/acs.joc.9b01194. Epub 2019 Aug 1.
A Ru-catalyzed -selective C-H nitration of 2-arylbenzothiazoles and 2-arylthiazoles has been developed. A wide range of functional groups are tolerated, providing the -nitrated products in good to excellent yields using Cu(NO)·3HO as the nitro source. The nitration could be carried out on a gram scale and used for the synthesis of promising therapeutic leads for human African trypanosomiasis.
发展了一种 Ru 催化的 2-芳基苯并噻唑和 2-芳基噻唑的 -选择性 C-H 硝化反应。该反应能够耐受多种官能团，以 Cu(NO)·3HO 作为硝基源，以良好至优秀的产率得到 -硝化产物。该硝化反应可以进行克级规模的实验，并且可以用于合成治疗人类非洲锥虫病的有前景的治疗先导化合物。
