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

被引：30

作者：

Bao, Yapeng ^{[1
]}

Deng, Zongfa ^{[1
]}

Feng, Jing ^{[1
]}

Zhu, Weiwei ^{[1
]}

Li, Jin ^{[1
]}

Wan, Jinqiao ^{[1
]}

Liu, Guansai ^{[1
]}

机构：

[1] HitGen Inc, Discovery Chem Unit, Chengdu 610200, Sichuan, Peoples R China

来源：

ORGANIC LETTERS | 2020年 / 22卷 / 16期

关键词：

N BOND FORMATION; CHEMICAL LIBRARIES; INHIBITORS; DESIGN; CYCLIZATION; POTENT;

D O I：

10.1021/acs.orglett.0c02032

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

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-2(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.

引用

页码：6277 / 6282

页数：6

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