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Updated: Jun 6, 2026

A Two-Step Protocol for Umpolung Functionalization of Ketones Via Enolonium Species
Published on: August 16, 2018
Conversion of Diverse Aromatic Amines to 3-Acyl-Substituted Pyridine/Pyrimidine-Fused Heterocyclic Derivatives via
Yu-Jia Fan1, You Zhou2, Yu-Man Song1
1State Key Laboratory of Green Pesticide, International Joint Research Center for Intelligent Biosensor Technology and Health, College of Chemistry, Central China Normal University, Wuhan 430079, P. R. China.
Abstract:
We describe a modular strategy for synthesizing seven types of 3-acyl-substituted fused pyridine and pyrimidine derivatives via an iodine-mediated, multicomponent tandem [3 + 1 + 2] annulation. This reaction employs rongalite and enaminones as C1 and C2 synthons and exhibits broad compatibility with various aromatic amines. The method offers significant advantages, including metal-free catalysis, simple operation, readily available starting materials, and high efficiency. Herein, we emphasize the versatility and divergent synthetic utility of this strategy, positioning it as a strategic extension for the construction of pyridine- and pyrimidine-fused heterocyclic scaffolds.
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