期刊
ORGANIC CHEMISTRY FRONTIERS
卷 8, 期 14, 页码 3705-3711出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/d1qo00368b
关键词
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资金
- Science, Technology and Innovation Commission of Shenzhen [JCYJ20190809160211372, KQTD20150717103157174]
- National Natural Science Foundation of China [21991113]
- Shenzhen Clean Energy Research Institute [CERI-KY-2019-003]
- Guangdong Provincial Key Laboratory of Catalysis [2020B121201002]
A highly efficient method for the synthesis of chiral secondary 2,2,2-trifluoroethanols has been developed, providing high yields and excellent enantioselectivities. The practicality of this method was demonstrated through the facile preparation of key intermediates of Odanacatib and LX-1301.
Due to their stereoelectronic properties, trifluoromethyl (or perfluoroalkyl) ketones are challenging substrates in asymmetric (transfer) hydrogenation. We have developed iridium/f-amphol and iridium/f-ampha catalysis systems, which provide a highly efficient method for the synthesis of chiral secondary 2,2,2-trifluoroethanols in high yields (up to 99%) with excellent enantioselectivities (up to 99% ee). The practicability of this methodology was demonstrated through the facile preparation of the key intermediates of Odanacatib and LX-1301.
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