Recent advances in organocatalytic cascade reactions for enantioselective synthesis of chiral spirolactone skeletons

Chiral spirolactones, including spiropropyllactones, spirobutyrolactones, and spirovalerolactones, are important heterocyclic frameworks that attracted the attention of organic medicinal chemists because these motifs constitute core structure several natural products bioactive molecules. The absolute configuration substituents on fully substituted spirocyclic stereocenter lactone can potentially enhance specificity for ligand-protein binding bioavailability, potency, metabolic stability. So, intensive from has been paid to synthetic methods leading such prominent structural motifs. be divided into two main classes. first approach takes advantage presence existing focuses its functionalization. second is framework constructed various precursors in a direct spirolactonization reaction. In this review, convenience reading, recent advances synthesis spirolactones summarized discussed according major organocatalytic asymmetric routes: (i) using lactone-related as building blocks; (ii) reaction reagents. This review also describes both mechanisms related transformations, gives some insights challenging issues research field, which will enlighten future development field.