27-Jul-2026
New catalytic strategy delivers chiral three-dimensional molecular scaffolds for future medicines
Science Exploration Press
Medicinal chemists are increasingly exploring saturated, three-dimensional bioisosteres as alternatives to planar aromatic heterocycles to improve the physicochemical and pharmacological properties of drug candidates. Among these emerging molecular frameworks, 3-azabicyclo[3.1.1]heptanes (3-aza-BCHeps) have attracted growing interest as potential pyridine bioisosteres. However, catalytic enantioselective methods for accessing these chiral nitrogen-bridged scaffolds have remained scarce. Researchers have now developed a chiral Brønsted acid-catalyzed asymmetric transfer hydrogenation that provides efficient access to enantioenriched 3-aza-BCHeps with broad substrate scope and excellent enantioselectivity.
- Journal
- Chiral Chemistry
- Funder
- National Natural Science Foundation of China, National Natural Science Foundation of China, National Natural Science Foundation of China, National Natural Science Foundation of China, National Key Research and Development Program of China, Guangdong Basic and Applied Basic Research Foundation, Guangdong Basic and Applied Basic Research Foundation, Shenzhen Science and Technology Program, High Level of Special Funds