Yapeng Bao; Zongfa Deng; Jing Feng; Weiwei Zhu; Jin Li; Jinqiao Wan; Guansai Liu
Org. Lett., 2020, 22(16), 6277-6282
https://doi.org/10.1021/acs.orglett.0c02032

Abstract

Indazolone cores are among the most common structural components in medicinal chemistry and can be found in many biologically active molecules. In this report, a mild and efficient approach to 2-substituted indazolones via B2(OH)4-mediated reductive N–N bond formation is developed. This strategy features mild conditions, no request for a metal catalyst, and a wide scope for both aliphatic and aromatic amines. Meanwhile, this method was further successfully applied on DNA to construct indazolone cores for a DNA-encoded library. This will enable the production of a very attractive indazolone-cored library from simple amines and scaffolds, which will provide considerable diversity.