A B<sub>2</sub>(OH)<sub>4</sub>‑Mediated Synthesis of 2‑Substituted Indazolone and Its Application in a DNA-Encoded Library

Published on 2020-08-01T19:13:41Z (GMT) by
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 B<sub>2</sub>(OH)<sub>4</sub>-mediated reductive <i>N</i>–<i>N</i> 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.

Cite this collection

Bao, Yapeng; Deng, Zongfa; Feng, Jing; Zhu, Weiwei; Li, Jin; Wan, Jinqiao; et al. (2020): A B2(OH)4‑Mediated Synthesis

of 2‑Substituted Indazolone and Its Application in a DNA-Encoded

Library. ACS Publications. Collection. https://doi.org/10.1021/acs.orglett.0c02032