Synthesis of P‐Stereogenic Compounds by Transition Metal‐Catalyzed Asymmetric Transformation of H−P(O) Compounds: Progress, Challenges, and Prospects

Abstract The synthesis of P‐stereogenic phosphorus compounds has gained considerable attention due to their wide applications across many research fields. Among the available strategies, transition metal‐catalyzed asymmetric transformation of pentavalent phosphoryl (H−P(O)) precursors is particularly appealing. This approach involves a direct C−P bond‐forming process, rendering it straightforward, and it employs readily available, bench‐stable H−P(O) reagents that are compatible with various metal catalysts. Recent years have witnessed significant progress in this field, with a primary focus on asymmetric C−P cross‐couplings and hydrophosphorylations. This Concept article provides a brief summary of recent progress, highlights existing challenges, and discusses future directions in this exciting area.