Access to planar chiral molecules remains a longstanding challenge in asymmetric synthesis. Enantiopure 2.2paracyclophanes are particularly attractive due to their broad applications in medicinal chemistry, asymmetric catalysis, and materials science. Herein, we present a highly stereoselective approach for the desymmetrization of prochiral pseudo ‐ para diformyl2.2paracyclophanes, enabled by chiral Brønsted acid‐catalyzed reductive amination. This method furnishes planar chiral structures with excellent enantiocontrol and broad substrate scope. Moreover, the resulting products can be readily modified, underscoring the utility of this approach as a versatile platform for the asymmetric synthesis of planar chiral 2.2paracyclophane derivatives.
Shinde et al. (2026) studied this question.