ol0c02032_si_001.pdf (5.32 MB)
A B2(OH)4‑Mediated Synthesis of 2‑Substituted Indazolone and Its Application in a DNA-Encoded Library
journal contribution
posted on 2020-08-01, 19:13 authored by Yapeng Bao, Zongfa Deng, Jing Feng, Weiwei Zhu, Jin Li, Jinqiao Wan, Guansai LiuIndazolone 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.