芳烃和烯烃的C-H区域选择性硫属化合和卤素化反应在无金属条件下进行。
Regioselective C-H chalcogenylation and halogenation of arenes and alkenes under metal-free conditions.
发表日期:2023 Mar 21
作者:
Bin Li, Mingli Hu, Jun Ge, Wei Xu, Jinghan Wu, Yao Tong, Zhengyi Zhao, Xiuxiu Liu, Ling He
来源:
Cellular & Molecular Immunology
摘要:
这篇论文报道了在无导向基和无金属条件下,在PIFA作用下直接对N-芳基吡咯酮进行Csp2-H硫、硒化和卤化反应。使用二苯硒/硫和苯硒卤化物作为反应试剂,分别得到硫、硒芳基化和卤芳基化的N-芳基吡咯酮产物。机理研究表明,在这些反应中可能涉及自由基途径。初步抗肿瘤实验显示,这些化合物在体外对人类急性白血病细胞K562具有中度至强的活性,可用作后续研究的先导化合物。
The reactions of direct Csp2-H chalcogenylation and halogenation of N-arylpyrrolidone under the action of PIFA without a directing group and under metal-free conditions were reported in this paper. Diphenyl selenide/sulfur and selenium phenyl halides were used as reaction reagents to obtain chalcogenylated and halogenated N-arylpyrrolidone products, respectively. The mechanistic studies indicated that a radical pathway was likely involved in these reactions. Preliminary antitumor tests showed that these compounds have moderate to potent activities against human acute leukemia cells K562 in vitro, which may be used as lead compounds for subsequent research.