Publication:
Glycosyl Triazole Based Pyridinamide/CuI-Catalyzed Coupling of 2-Halobenzamides with Active Methylene Compounds

Loading...
Thumbnail Image

Date

2023

Journal Title

Synthesis (Germany)

Journal ISSN

Volume Title

Publisher

Georg Thieme Verlag

Research Projects

Organizational Units

Journal Issue

Abstract

This report describes a convenient method for the Cu(I)- catalyzed tandem synthesis of dihydrophenanthridinediones and substituted isoquinolinones with the assistance of efficient glycosyl 1,2,3-triazole-based pyridinamide ligands. The catalytic system effectively works for the coupling of N-substituted 2-halobenzamides with various active methylene compounds to form biologically relevant heterocyclic scaffolds in high to excellent yields. The consecutive path of the reaction including intermolecular C C cross-coupling followed by intramolecular cyclization efficiently takes place at low catalytic loading. These glycosyl triazole-appended pyridinamides were synthesized in good yields by a CuI/DIPEA-mediated regioselective CuAAC click reaction. The notable features of the method include low catalytic loading, the use of cost-effective and biocompatible ligands, high reaction yield, and easily accessible starting materials that make the protocol more versatile. � 2023 Georg Thieme Verlag. All rights reserved.

Description

Keywords

carbohydrates, copper catalysis, cross-coupling, CuAAC click reaction, glycohybrids, triazoles

Citation

Collections