Catalytic Asymmetric Synthesis of Spiropyrazolones and their Application in Medicinal Chemistry

Abstract Chiral spiropyrazolones are unique frameworks widely found in a large family of medicinally relevant compounds with various biological activities. Substantial research efforts have been invested toward stereoselectively by constructing spiro‐cyclic structures. Over the past years, remarkable progress has been made in the organo‐ and metal‐catalyzed asymmetric synthesis of spiropyrazolones through the utilization of accessible simple pyrazolone derivatives as raw materials. This review is organized according to the size of the spiro‐ring fused at the 4‐position of the pyrazolone framework. In the last part, the bio‐evaluations of chiral spiropyrazolones for drug discovery are summarized.