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Updated: Mar 27, 2026

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[3 + 1 + 2] Annulation for Modular Synthesis of Polysubstituted Pyridines Using Calcium Carbide as an Acetylene
Botao Wang1, Ting Shao1, Jinhui Yang2
1College of Chemistry and Chemical Engineering, Northwest Normal University, Lanzhou, Gansu 730070, P. R. China.
Abstract:
A [3 + 1 + 2] annulation strategy for the modular synthesis of polysubstituted pyridines, such as 2,6-diarylnicotinic acid esters and nicotinonitriles, is described. Multicomponent reactions employ β-enamine esters/β-enamine nitriles and aromatic aldehydes as starting materials, and calcium carbide as a source of alkyne. The key advantages of this method include the use of an inexpensive and easy-to-handle solid alkyne source instead of flammable and explosive gaseous acetylene, a broad substrate scope with good functional group tolerance, high yield, operational simplicity, and scalability to the gram scale.
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