Asymmetric Cycloaddition/Annulation Reactions by Chiral Phosphoric Acid Catalysis: Recent Advances

Abstract Asymmetric cycloaddition/annulation reactions have contributed greatly to the synthesis of a variety of novel cyclic compounds used in organic synthesis, natural product synthesis, material science, and chemical biology. Thus, chiral phosphoric acid‐catalyzed asymmetric cycloaddition reactions have received the attention of the synthetic community to design new vital asymmetric reactions and synthesize complex molecules for the past two decades. Although several review articles on organocatalyzed asymmetric cycloaddition reactions can be found in the literature, there has been no specific review on CPA‐catalyzed asymmetric cycloaddition/annulation reactions. Herein, the most recent research progress on chiral phosphoric acid catalyzed asymmetric [3+2], [4+2], [2+2], [3+3], [4+3], [4+1] annulation, and 1,3‐dipolar cycloadditions have been compiled and analyzed to demonstrate the importance of chiral phosphoric acid catalysis in asymmetric cycloaddition or annulation reactions.