Recent Advances in the Synthesis of 1,4‐Enynes and Their Applications in Organic Synthesis

The chemistry of 1,n‐enynes, especially 1,4‐enynes, represents a privileged scaffold in organic synthesis, constituting both the core structural units of numerous natural products and bioactive molecules and serving as a versatile substrate for diverse transition metal‐catalyzed cyclization transformations. Over the past few decades, the synthesis of 1,4‐enynes and their application in constructing fused and spirocyclic frameworks have attracted considerable research attention. These synthetic methods offer great promise for the assembly of diverse complex molecules, including pharmaceuticals, natural products, agrochemicals, and functional materials. In this review, recent advances in the synthesis of 1,4‐enynes and their chemical transformations with diverse coupling reagents are summarized. Meanwhile, mechanistic studies, supported by experimental investigations, are discussed to illuminate the synergistic interactions governing bond formation. The practical utility of these methodologies is further demonstrated through their application in the synthesis of complex natural products and pharmaceutical intermediates, highlighting their potential for scalable and sustainable chemical manufacturing.