10.1021/acs.orglett.0c02032.s001
Yapeng Bao
Yapeng
Bao
Zongfa Deng
Zongfa
Deng
Jing Feng
Jing
Feng
Weiwei Zhu
Weiwei
Zhu
Jin Li
Jin
Li
Jinqiao Wan
Jinqiao
Wan
Guansai Liu
Guansai
Liu
A B<sub>2</sub>(OH)<sub>4</sub>‑Mediated Synthesis
of 2‑Substituted Indazolone and Its Application in a DNA-Encoded
Library
American Chemical Society
2020
DNA-Encoded Library Indazolone cores
B 2
Mediated
indazolone-cored
diversity
amines
scaffold
strategy
reductive
Application
2-
approach
method
Synthesi
Substituted
indazolone
molecule
component
DNA-encoded
formation
catalyst
scope
aliphatic
OH
bond
2020-08-01 19:13:41
Journal contribution
https://acs.figshare.com/articles/journal_contribution/A_B_sub_2_sub_OH_sub_4_sub_Mediated_Synthesis_of_2_Substituted_Indazolone_and_Its_Application_in_a_DNA-Encoded_Library/12751096
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.