Recent advances in the applications of pyrazolone derivatives in enantioselective synthesis

Pyrazolones and pyrazoles, featuring nitrogen-nitrogen bonds, are two of the most important classes of heterocycles, owing to their widespread occurrence in medicinal chemistry and functional materials. The last decade has witnessed a rapid increase in the construction of chiral pyrazolone and pyrazole derivatives, with the application of pyrazolone derivatives as powerful synthons. Since our last review in 2018, a large number of new achievements has emerged in this area, requiring a timely update. Thus, this review summarizes these elegant achievements based on the multiple reactive sites of different pyrazolone synthons. In addition, important mechanisms and interesting biological investigations relating to the corresponding products are also discussed.

Automated summary

Pyrazolones and pyrazoles, important heterocyclic compounds, have wide applications in medicinal chemistry and functional materials. In the past decade, there has been a rapid increase in the study of chiral pyrazolone and pyrazole derivatives, which serve as powerful synthons. This review summarizes recent achievements in this field, focusing on the multiple reactive sites of different pyrazolone synthons. The review also discusses important mechanisms and interesting biological investigations related to the corresponding products.