Welcome to HitGen

About

Enable Innovative Drug Discover with DEL, FBDD and SBDD

  1. 关于我们
  2. Publications

A B2(OH)4-Mediated Synthesis of 2-Substituted Indazolone and Its Application in a DNA-Encoded Library 发布时间:2020-08-01

Abstract:

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.


Org. Lett. 2020, 22, 16, 6277–6282

https://doi.org/10.1021/acs.orglett.0c02032

Link:https://pubs.acs.org/doi/10.1021/acs.orglett.0c02032

Thanks for reading!

For more details on how we can advance your innovative drug discovery projects
验证码
By submitting your information, you acknowledge having received, read and understood our Privacy Notice as made available above.

We use cookies to provide a better web experience.
By using our site, you acknowledge our use of cookies and please read our Cookie Notice for More information