Thieme Chemistry
Highly Evaluated Publications
in Chemical Synthesis
Thieme Chemistry期刊 Synthesis 和 Synlett 最新一期全新上线。本期两本期刊的封面论文全部来自中国作者，其中Synthesis的封面论文来自江西师范大学国家单糖化学合成工程技术研究中心胡祥国教授及其同事；Synlett的封面论文来自苏州大学材料与化学化工学部朱晨教授及其同事。欢迎阅读两篇封面论文及本期的其它论文。
Issue 04 · Volume 32 · March 2021
封面论文
Radical-Mediated Hetaryl Functionalization of Nonactivated Alkenes through Distal ipso-Migration of O- or S-Hetaryls
Huihui Zhang, Meishan Ji, Youhao Wei, Haodong Chen, Xinxin Wu, Chen Zhu
苏州大学 材料与化学化工学部
A radical-mediated hetaryl functionalization of nonactivated alkenes through distal ipso-migration of O- or S-containing hetaryls was developed. Furyl, benzofuryl, thienyl, and benzothienyl groups showed satisfactory migratory abilities. A variety of heteroatom-centered radicals, including azido, trifluoromethylsulfanyl, and silyl radicals readily trigger the migration cascade, and a new C–heteroatom and C–C bond are concomitantly constructed in the reaction. This method provides an efficient approach to the synthesis of high-valued complex O- or S-hetaryl compounds.
Issue 06 · Volume 53 · March 2021
封面论文
Late-Stage Transformation of Carboxylic Acids to N-Trifluoroethylimides with Trifluoromethyl Diazomethane
Xiao-Feng Qiu, De-Yong Liu, Wen-Feng Zhang, Xiang-Guo Hu
江西师范大学国家单糖化学合成工程技术研究中心
We report the first systematic evaluation of the reaction of trifluoromethyl diazomethane (2,2,2-trifluorodiazoethane, CF3CHN2) with drug-like molecules. We found our previous copper-catalyzed transformation of carboxylic acids to the corresponding N-trifluoroethylimides with CF3CHN2 and acetonitrile is well-suited for the late-stage modification of drug and drug-like acids. A procedure that enables the use of solid nitriles and nitriles with high boiling points as viable substrates is also disclosed.
