title: Regioselective Synthesis of N-Heteroaromatic Trifluoromethoxy Compounds by Direct O-CF3 Bond Formation.
abstract: The first one-step method for the synthesis of ortho-N-heteroaromatic trifluoromethoxy derivatives by site-specific O-CF3 bond formation using hydroxylated N-heterocycles and Togni's reagent is described. The approach enables the unprecedented syntheses of a wide range of six or five-membered N-heteroaromatic trifluoromethoxy compounds containing one or two heteroatoms from most commonly used hydroxylated N-heterocycles. Notable advantages of this method include its simplicity and mild conditions, avoidance of the need for metals or toxic reagents, and compatibility with a variety of functional groups. Furthermore, this method is especially suitable for the larger scale application.
authors.affiliation: The College of Chemistry and Molecular Engineering, Zhengzhou University, Zhengzhou, 450001, P. R. China.|Tetranov Biopharm, LLC and Collaborative Innovation Center of New Drug Research and Safety Evaluation, Henan Province, No. 75 Daxue Road, Zhengzhou, 450052, P. R. China.
authors.forename: Apeng
authors.initials: A
authors.lastname: Liang
authors.affiliation: The College of Chemistry and Molecular Engineering, Zhengzhou University, Zhengzhou, 450001, P. R. China.
authors.forename: Shuaijun
authors.initials: S
authors.lastname: Han
authors.affiliation: The College of Chemistry and Molecular Engineering, Zhengzhou University, Zhengzhou, 450001, P. R. China.
authors.forename: Zhenwei
authors.initials: Z
authors.lastname: Liu
authors.affiliation: The College of Chemistry and Molecular Engineering, Zhengzhou University, Zhengzhou, 450001, P. R. China.
authors.forename: Liang
authors.initials: L
authors.lastname: Wang
authors.affiliation: The College of Chemistry and Molecular Engineering, Zhengzhou University, Zhengzhou, 450001, P. R. China.|Tetranov Biopharm, LLC and Collaborative Innovation Center of New Drug Research and Safety Evaluation, Henan Province, No. 75 Daxue Road, Zhengzhou, 450052, P. R. China.
authors.forename: Jingya
authors.initials: J
authors.lastname: Li
authors.affiliation: The College of Chemistry and Molecular Engineering, Zhengzhou University, Zhengzhou, 450001, P. R. China. zdp@zzu.edu.cn.|Tetranov Biopharm, LLC and Collaborative Innovation Center of New Drug Research and Safety Evaluation, Henan Province, No. 75 Daxue Road, Zhengzhou, 450052, P. R. China. zdp@zzu.edu.cn.
authors.forename: Dapeng
authors.initials: D
authors.lastname: Zou
authors.affiliation: The College of Chemistry and Molecular Engineering, Zhengzhou University, Zhengzhou, 450001, P. R. China. wyj@zzu.edu.cn.
authors.forename: Yangjie
authors.initials: Y
authors.lastname: Wu
authors.affiliation: The College of Chemistry and Molecular Engineering, Zhengzhou University, Zhengzhou, 450001, P. R. China. yusheng.wu@tetranovglobal.com.|Tetranov Biopharm, LLC and Collaborative Innovation Center of New Drug Research and Safety Evaluation, Henan Province, No. 75 Daxue Road, Zhengzhou, 450052, P. R. China. yusheng.wu@tetranovglobal.com.|Tetranov International, Inc., 100 Jersey Avenue, Suite A340, New Brunswick, NJ, 08901, USA. yusheng.wu@tetranovglobal.com.
authors.forename: Yusheng
authors.initials: Y
authors.lastname: Wu
keywords: C−O bond formation; N-heterocycles; hypervalent iodine reagents; trifluoromethylation