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Updated: Aug 23, 2025

Enzymatic Cascade Reactions for the Synthesis of Chiral Amino Alcohols from L-lysine
Published on: February 16, 2018
Highly efficient and enantioselective synthesis of β-heteroaryl amino alcohols via Ru-catalyzed asymmetric
Chao Wu1,2, Baode Ma2, Gen-Qiang Chen3
1School of Chemistry and Chemical Engineering, Harbin Institute of Technology, Harbin, 150001, People's Republic of China.
Abstract:
Chiral β-heteroaryl amino alcohols are key fragments of many bioactive compounds and antibiotics, and the development of efficient synthetic methods for these compounds is of great value. The highly enantioselective hydrogenation of α-N-heteroaryl ketones was realized with a ruthenium-diphosphine-diamine catalyst, providing the corresponding chiral β-heteroaryl amino alcohols with up to 99% yield and up to >99% ee. The synthetic utilities of the current reaction were demonstrated by gram-scale synthesis of key intermediates of Sertaconazole and Cenobamate.
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