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2-取代吲唑酮衍生物的快速且与卤化物兼容的合成——水相介质中的光化学环化反应

Rapid and halide compatible synthesis of 2--substituted indazolone derivatives photochemical cyclization in aqueous media.

作者信息

Nie Hui-Jun, Guo An-Di, Lin Hai-Xia, Chen Xiao-Hua

机构信息

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

出版信息

RSC Adv. 2019 Apr 30;9(23):13249-13253. doi: 10.1039/c9ra02466b. eCollection 2019 Apr 25.

Abstract

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.

摘要

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。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7b50/9063774/40863d3f90fd/c9ra02466b-s1.jpg

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