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

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

doi:10.1039/c9ra02466b

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

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

Authors

Hui-Jun Nie^{1

2}, An-Di Guo², Hai-Xia Lin¹, Xiao-Hua Chen²

Affiliations

¹ Department of Chemistry, Innovative Drug Research Center, College of Sciences Shanghai University Shanghai 200444 China.
² 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 xhchen@simm.ac.cn.

Abstract

Indazolone derivatives exhibit a wide range of biological and pharmaceutical properties. We report a rapid and efficient approach to provide structurally diverse 2-N-substituted indazolones via 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.