2-取代吲唑的无金属区域选择性单卤化和多卤化反应
Metal-free regioselective mono- and poly-halogenation of 2-substituted indazoles.
作者信息
Zhang Changjun, Wei Tingting, Yu Zhichen, Ding Yuxin, Su Weike, Xie Yuanyuan
机构信息
College of Pharmaceutical Sciences, Zhejiang University of Technology Hangzhou 310014 P. R. China
Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaeuticals, Zhejiang University of Technology Hangzhou 310014 P. R. China.
出版信息
RSC Adv. 2023 Feb 7;13(8):4958-4962. doi: 10.1039/d2ra07398f. eCollection 2023 Feb 6.
An unprecedented metal-free regioselective halogenation of 2-indazoles has been revealed, which not only realized the highly selective synthesis of mono-halogenated products, but also completed poly-halogenations by fine tuning the reaction conditions. Various mono-/poly-/hetero-halogenated indazoles were obtained in moderate to excellent yields. Notably, this approach features environmentally friendly solvents, mild reaction conditions, simple execution and short reaction time.
已揭示了一种前所未有的2-吲唑的无金属区域选择性卤化反应，该反应不仅实现了单卤代产物的高选择性合成，还通过微调反应条件完成了多卤化反应。以中等到优异的产率获得了各种单卤代/多卤代/杂卤代吲唑。值得注意的是，该方法具有环境友好的溶剂、温和的反应条件、操作简单和反应时间短的特点。
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