Desymmetrization strategy in natural product total synthesis

Desymmetrization strategies have emerged as practical methods for the efficient construction of desired molecules from readily accessible symmetrical precursors. This approach has found widespread application in natural product total synthesis as it simplifies the materials preparation, enables the precise control of chirality formation, and inspires innovative retrosynthetic analysis. Here, we summarize recent advances (2014–2024) of the applications of desymmetrization strategies in natural product total synthesis, and showcase their advantages in designing new reactions and synthetic strategies, with the aim to foster their wider application in total synthesis.