1,3-Diynes: A Versatile Precursor in Transition-Metal Catalyzed (Mediated) C-H Functionalizations.

Transition metal-catalyzed C-H functionalization of diverse arenes with alkyne units has attracted enormous attention for decades since they provide straightforward access to various functionalization/annulations, which are commonly present in bioactive compounds and natural products. Recently, conjugated alkynes (1,3-diynes) have been utilized as key coupling partner in many C-H activation reactions due to their versatile characteristic properties. The presence of two C≡C bonds in conjugated 1,3-diyne brings the new diversity in synthetic transformations, such as chemo-, regioselective pathways, mono-bis functionalizations, cascade annulations, etc. Herein, we summarized the latest developments in the realm of transition-metal-catalyzed C-H functionalizations of diverse arenes with 1,3-diynes. Moreover, we highlighted the diverse transformations, conditions, mechanisms and applications of the corresponding reaction in detail.