A Facile Synthesis of Indole Derivatives by a Palladium‐Catalyzed Process Initiated from Ugi Adducts and their Antifungal Activities

In this work, an efficient synthesis of indole derivatives through palladium‐catalyzed double isocyanide insertion reactions has been developed. The reaction intermediates could be readily obtained by Ugi reactions. The transformation features broad functional‐group compatibility, commercially avail...

Full description

Saved in:
Bibliographic Details
Published in:ChemistrySelect (Weinheim) 2021-12, Vol.6 (45), p.12921-12925
Main Authors: Qiu, Ji‐Ying, Yuan, Ding, Yu, Jing‐Jing, Zhang, Yi, Li, Wen‐Hao, Tang, Zeng‐Xiang, He, Ping, Ren, Zhi‐Lin
Format: Article
Language:English
Subjects:
antifungal activities
indole derivatives
isocyanide insertion
Pd-catalyzed reaction
Ugi reactions
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:In this work, an efficient synthesis of indole derivatives through palladium‐catalyzed double isocyanide insertion reactions has been developed. The reaction intermediates could be readily obtained by Ugi reactions. The transformation features broad functional‐group compatibility, commercially available starting materials, and moderate to good reaction yields. Furthermore, the bioactivities of the synthesized compounds were evaluated in mycelial growth tests against Penicilium digitatum and Colletotrichun gloeosporioides, and showed potential antifungal activities. Herein, we have disclosed a concise access to the construction of indole derivatives by Pd‐catalyzed double isocyanide insertion reactions initiated from classical Ugi reactions in moderate to good yields. The broad functional‐group compatibility and available starting materials make this method a valuable tool for generating diverse indole derivatives, which are of considerable interest in synthetic and medicinal chemistry. Furthermore, the bioactivities of the synthesized compounds were evaluated against Penicilium digitatum and Colletotrichun gloeosporioides, and showed potential antifungal activities.
ISSN:2365-6549
2365-6549
DOI:10.1002/slct.202104070