Nie Hui-Jun, Guo An-Di, Lin Hai-Xia, Chen Xiao-Hua
Department of Chemistry, Innovative Drug Research Center, College of Sciences Shanghai University Shanghai 200444 China.
Chinese Academy of Sciences Key Laboratory of Receptor Research, Synthetic Organic & Medicinal Chemistry Laboratory, Shanghai Institute of Materia Medica, Chinese Academy of Sciences Shanghai 201203 China
RSC Adv. 2019 Apr 30;9(23):13249-13253. doi: 10.1039/c9ra02466b. eCollection 2019 Apr 25.
Indazolone derivatives exhibit a wide range of biological and pharmaceutical properties. We report a rapid and efficient approach to provide structurally diverse 2--substituted indazolones photochemical cyclization in aqueous media at room temperature. This straightforward protocol is halide compatible for the synthesis of halogenated indazolones bearing a broad scope of substrates, which suggests a new avenue of great importance to medicinal chemistry.
吲唑酮衍生物具有广泛的生物学和药学性质。我们报道了一种快速有效的方法，可在室温下于水性介质中通过光化学环化反应提供结构多样的2-取代吲唑酮。这种直接的方案与卤化物兼容，可用于合成具有广泛底物范围的卤代吲唑酮，这为药物化学开辟了一条非常重要的新途径。
