Recent Applications of the Sonogashira Reaction in the Synthesis of Drugs and Their Derivatives: A Review

ABSTRACT Metal‐catalyzed cross‐coupling reactions are essential tools for constructing C–C bonds in organic synthesis. Among these prominent approaches, the Sonogashira reaction stands out as a key player and is widely utilized in medicinal chemistry. This versatile method enables the creation of complex C (sp2)–C (sp) bonds by linking aryl or vinyl halides with terminal alkynes, facilitating the efficient construction of molecular structures crucial for drug development. A notable application of the Sonogashira reaction is its ability to incorporate aromatic and alkynyl functionalities into pharmaceutical compounds. Depending on the impactful catalytic system evolved gradually, the Sonogashira reaction can involve either double‐metal catalysis or single‐metal catalysis. This review sheds light on the diverse applications of the Sonogashira coupling approach in drug synthesis and the generation of their derivatives. The review is thoughtfully organized around the catalytic systems in use, delineating between double‐metal catalysis and single‐metal catalysis for better clarity. Encompassing a range of applications, this thorough summary delves into the diverse ways in which the Sonogashira reaction has been leveraged in pharmaceutical synthesis and its derivatives in recent times.