Tetrahedron letters2022，Vol.966.DOI:10.1016/j.tetlet.2022.153732

DNA-encoded focused indazole library synthesis by a palladium- mediated C-N(sp(2)) cross-coupling reaction between DNA-linked (hetero)aryl halides and aromatic nitrogen heterocycles

Yang, Juan Xia, Shengdi Liu, Jiaxiang Yu, Zikun Mei, Lianghe Lu, Weiwei Chen, Yulin Chen, Shaopeng Wang, Xuan Lu, Xiaojie
Tetrahedron letters2022，Vol.966.DOI:10.1016/j.tetlet.2022.153732
✕
  • NSTL
  • Elsevier

DNA-encoded focused indazole library synthesis by a palladium- mediated C-N(sp(2)) cross-coupling reaction between DNA-linked (hetero)aryl halides and aromatic nitrogen heterocycles

Yang, Juan 1Xia, Shengdi 2Liu, Jiaxiang 3Yu, Zikun 3Mei, Lianghe 1Lu, Weiwei 1Chen, Yulin 1Chen, Shaopeng 1Wang, Xuan 1Lu, Xiaojie1
扫码查看

作者信息

  • 1. Chinese Acad Sci
  • 2. Nanjing Univ Chinese Med
  • 3. Alphama Biotechnol Suzhou Co Ltd
  • 折叠

Abstract

Incorporating various heteroaryl motifs into small-molecule moieties of DNA-encoded libraries is beneficial to support hit identification. More privileged heterocycles based libraries are urgently needed to expand the chemical space of the DNA encoded library. Because currently published on-DNA C-N cross-coupling methods mainly focused on exocyclic aromatic amines, lacking systematic investigation for incorporating pharmaceutically valuable N-aryl hetero-aromatic moiety into DNA-encoded libraries, in this paper, we have reported an on-DNA protocol to attach the DNA-linked electrophiles to the (H)N- heteroaryl rings. This method could translate the monofunctional heteroaryl agents into "bifunctional building blocks ", which have been applied for the DNA encoded focused indazole library synthesis. (C) 2022 Elsevier Ltd. All rights reserved.

Key words

ARYLATION/CHEMISTRY/BROMIDES/PD

引用本文复制引用

出版年

2022
Tetrahedron letters

Tetrahedron letters

CCR
ISSN：0040-4039
被引量3
参考文献量19
段落导航相关论文