The majority of drugs work by interacting with chiral counterparts, such as proteins, and we are all too aware of how chirality can have a negative impact on the outcome of a therapeutic regimen. The market for chiral, non-racemic drugs is growing, and it is becoming increasingly important to prepare these compounds in a safe, cost-effective, and environmentally sustainable manner. Asymmetric organocatalysis has a long history, but its renaissance period began only in the first millennium. Since then, this field has advanced to an extraordinary level, as evidenced by the awarding of the 2021 Nobel Prize in Chemistry. We would like to highlight the use of organocatalysis in the synthesis of enantio-enriched molecules that may be of interest to the pharmaceutical industry and the medicinal chemistry community in this review.
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