Journal
ORGANIC LETTERS
Volume 22, Issue 11, Pages 4322-4326Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.0c01361
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Funding
- State Key Laboratory of Anti-Infective Drug Development (Sunshine Lake Pharma Co., Ltd) [2015DQ780357]
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A method for the enantioselective synthesis of cis-3-quinuclidinols by Ru-catalyzed asymmetric transfer hydrogenation via dynamic kinetic resolution is described. The reaction proceeded under mild conditions using ammonium formate as the hydrogen donor, affording the products in high yields (up to 99%) with excellent diastereoselectivity (up to 99:1 dr) and enantioselectivity (95-99% ee). This protocol was applicable to gram-scale preparation with perfect enantioselectivity through simple recrystallization.
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