期刊
ORGANIC PROCESS RESEARCH & DEVELOPMENT
卷 22, 期 1, 页码 103-107出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.oprd.7b00376
关键词
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资金
- German Research Foundation [ME 1805/15-1]
The catalytic, enantioselective synthesis of key propargylic alcohol intermediates toward the synthesis of the anti-HIV drug efavirenz is reported. Using a recently reported chiral-at-ruthenium catalyst (J. Am. Chem. Soc. 2017, 139, 4322), catalytic enantioselective alkynylations of 1-(2,5-dichlorophenyl)-2,2,2-trifluoroethanone (99% yield, 95% ee) and 1-(5-chloro-2-nitrophenyl)-2,2,2-trifluoroethanone (97% yield, 99% ee) are achieved using catalyst loadings of merely 0.2 mol % (ca. 500 TON).
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