2021/01/01 by Bo Han, Xiang‐Hong He, Yanqing Liu +3 · 1 citation
Biochemistry, Genetics and Molecular Biology · Chemistry · #Asymmetric Synthesis and Catalysis #Chemical Synthesis and Analysis #Chemical Synthesis and Reactions
paper · doi:10.1039/d0cs00196a
openalex publication_date 2021/01/01 · openalex created_date 2025/10/10 · openalex updated_date 2026/07/30
The efficacy and synthetic versatility of asymmetric organocatalysis have contributed enormously to the field of organic synthesis since the early 2000s. As asymmetric organocatalytic methods mature, they have extended beyond the academia and undergone scale-up for the production of chiral drugs, natural products, and enantiomerically enriched bioactive molecules. This review provides a comprehensive overview of the applications of asymmetric organocatalysis in medicinal chemistry. A general picture of asymmetric organocatalytic strategies in medicinal chemistry is firstly presented, and the specific applications of these strategies in pharmaceutical synthesis are systematically described, with a focus on the preparation of antiviral, anticancer, neuroprotective, cardiovascular, antibacterial, and antiparasitic agents, as well as several miscellaneous bioactive agents. The review concludes with a discussion of the challenges, limitations and future prospects for organocatalytic asymmetric synthesis of medicinally valuable compounds.