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

Yapeng Bao, Zongfa Deng, Jing Feng*, Weiwei Zhu, Jin Li, Jinqiao Wan* and Guansai Liu*

*Discovery Chemistry Unit, HitGen Inc., Building 6, No. 8 Huigu 1st East Road, Tianfu International Bio-Town, Shuangliu District, Chengdu 610200, Sichuan, P. R. China, Email: jq.wanhitgen.com, gs.liuhitgen.com

Y. Bao, Z. Deng, J. Feng, W. Zhu, J. Li, J. Wan, G. Liu, Org. Lett., 2020, 22, 6277-6282.

DOI: 10.1021/acs.orglett.0c02032

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Abstract

B₂(OH)₄-mediated reductive N-N bond formation enables an efficient approach to 2-substituted indazolones. This method offers mild conditions, no request for a metal catalyst, and a wide scope for both aliphatic and aromatic amines.

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Key Words

indazolones, tetrahydroxydiboron

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ID: J54-Y2020