In the pursuit of a coherent synthetic route for the synthesis of carbo- and heterocycles, 2-alkynylarylnitrile has been recognized as a useful and versatile building block in organic synthesis due to the dual capacity of this precursor to act with a nucleophilic of electrophilic nature. The alkynes implanted at the ortho position improved the reactivity of the substrate for tandem cyclization and annulations, which led to the synthesis of diverse and complex cyclic compounds. This mini review summarizes the literature on the synthetic transformations of 2-alkynylarylnitrile into biologically relevant heterocycles as well as carbocycles such as isoindoles, isoquinolines, naphthalenes, and indenones as well as building blocks for the synthesis of various natural products. We hope that this concise review will be a promissory entry for future research in this area.
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