A B2(OH)4‑Mediated Synthesis
of 2‑Substituted Indazolone and Its Application in a DNA-Encoded
Library
Posted on 2020-08-01 - 19:13
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.
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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
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AUTHORS (7)
YB
Yapeng Bao
ZD
Zongfa Deng
JF
Jing Feng
WZ
Weiwei Zhu
JL
Jin Li
JW
Jinqiao Wan
GL
Guansai Liu