A Novel Three‐Component Reaction of Halo‐Pyridines with Grignard Reagents

Новая трёхкомпонентная реакция галогенопиридинов с реактивами Гриньяра
Zhiwei Huang, Liang‐Qi Fang, Jinghua Li, Jian Wang, Dongping Cheng
2025-05-01

Grignard reagentsbipyridinium saltshalo-pyridinesthree-component reactiontransition metal-free
Abstract A novel three‐component reaction of halo‐pyridines with Grignard reagents under transition metal‐free conditions is developed. Chloro‐ and bromo‐pyridines are treated with BTC/DMAP at room temperature to form bipyridinium salts, which then react with Grignard reagents to yield three‐component coupling products. The obtained pyridines linked 1,4‐dihydropyridines may offer a good opportunity to discover new bioactive molecules.
1
A novel three-component reaction of halo-pyridines with Grignard reagents was developed under transition metal-free conditions.
2
Chloro- and bromo-pyridines are activated with BTC/DMAP at room temperature to form bipyridinium salts.
3
The bipyridinium salts react with Grignard reagents to produce three-component coupling products.
4
The reaction yields pyridines linked to 1,4-dihydropyridines, proposed as potential scaffolds for discovering new bioactive molecules.

Halo-pyridines undergoing a three-component reaction with Grignard reagents under transition metal-free conditions (via BTC/DMAP-formed bipyridinium salts)

Development and mechanism/outcome of the three-component coupling that converts chloro- and bromo-pyridines (via BTC/DMAP activation) and Grignard reagents into pyridines linked to 1,4-dihydropyridines (reaction scope and product formation)

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2025-05-01
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Zhiwei Huang
Liang‐Qi Fang
Jinghua Li
Jian Wang
Dongping Cheng
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