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Review | Regular issue | Vol 104, No. 2, 2022, pp.215-228
Published online, 15th September, 2021
DOI: 10.3987/REV-21-969
Total Synthesis of Natural Products and Medicinal Molecules via Chelation-Controlled Diastereoselective Hydride Reduction of Amino Ketones

Tian Jin,* Lu Zhao, Chichong Lu,* Zhe-Bin Zheng, and Won-Hun Ham*

*Antibiotics Research and Re-evaluation Key Laboratory of Sichuan Province, Sichuan Industrial Institute of Antibiotics, School of Pharmacy, Chengdu University, Chengdu 610106, People’s Republic of China


The chiral β-amino alcohols are widely presented in the natural products, privileged ligands, and medicinal molecules. In the past decades, the construction of anti-β-amino alcohols have attracted in the interest of synthetic chemists. A number of studies indicated that the chelation-controlled hydride reduction approach is straightforward for the preparation of anti-β-amino alcohol motifs in high yield with excellent diastereoselectivity and they can be used as chiral building block in the total synthesis of natural products and medicinal molecules. The aim of this review is to highlight application of chelation-controlled hydride reduction in total synthesis of natural products and medicinal molecules on the basis of a collection of recent literature studies.