AbstractEnantioselective synthesis, which yields one enantiomer in higher concentration or purity than the other, has transformed the production of flavonoids. Flavonoids, which are found in large quantities in nature and are known to exhibit a diverse array of physiological activities, are an ideal choice for enantioselective synthesis due to the significance of chirality in their therapeutic effects. Enantioselective synthesis is used in the medicinal, nutraceutical, and agrochemical sectors to produce flavonoids, which are useful in the development of novel therapeutics with improved effectiveness and fewer adverse reactions. The ability to obtain specific enantiomers of flavonoids facilitates the elucidation of biochemical strategies and the relationship between structure and activity, thereby providing avenues for tailored drug design and optimization. This review highlights the critical role that enantioselective synthesis plays in achieving the full potential of flavonoids for a variety of therapeutic and non‐therapeutic applications. It also discusses the challenges and prospects of enantioselective syntheses to create relevant classes of flavonoid monomers, emphasizing their applications in the field. The review focused on the synthetic methods for fabricating native flavonoids and their analogs, highlighting the critical role that enantioselective synthesis of flavonoids plays in maximizing their therapeutic potential for enhancing human health and wellbeing.