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A B2(OH)4‑Mediated Synthesis of 2‑Substituted Indazolone and Its Application in a DNA-Encoded Library

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journal contribution
posted on 01.08.2020, 19:13 by Yapeng Bao, Zongfa Deng, Jing Feng, Weiwei Zhu, Jin Li, Jinqiao Wan, Guansai Liu
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 NN 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.