Catalytic Asymmetric Synthesis of Spiropyrazolones and their Application in Medicinal Chemistry

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.