Synthesis of 4‐Indolyl‐5‐Aminopyrazoles via Catalytic Arylation of 5‐Aminopyrazoles With 2‐Indolylmethanols
A Brønsted acid-catalyzed arylation of 5-aminopyrazoles with 2-indolylmethanols was established, which effectively afforded 4-indolyl-5-aminopyrazoles in high yields (up to 98%). Biological evaluation demonstrates the promising application of these 4-indolyl-5-aminopyrazoles in medicinal chemistry. This reaction not only provides a novel class of biologically active 4-aryl-5-aminopyrazoles but also offers an efficient strategy for synthesizing 4-(five-membered heteroaryl)-5-aminopyrazoles.
Authors
- Tianya Liu (ORCID: https://orcid.org/0000-0002-5371-6497)
- Yu‐Chen Zhang (ORCID: https://orcid.org/0000-0002-8399-7824)
- Xue Jia (ORCID: https://orcid.org/0009-0003-6591-4284)
- Xu Chen (ORCID: https://orcid.org/0009-0008-5896-9910)
- Feng Jian Shi (ORCID: https://orcid.org/0000-0003-3922-0708)
- Yangjun Chen (ORCID: https://orcid.org/0000-0002-4991-9558)
Institutions
- Jiangsu Normal University (CN)
- Xuzhou Medical College (CN)
- Changzhou University (CN)
Publication Details
- Journal
- Chemistry - An Asian Journal
- Published
- 2025-10-28
- DOI
- https://doi.org/10.1002/asia.202500861
- Citations
- 1
- Primary Topic
- Synthesis of Indole Derivatives
- Type
- article
- Field-Weighted Citation Impact
- 0.94
Funders
- National Natural Science Foundation of China
- Government of Jiangsu Province
- Basic Research Program of Jiangsu Province