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摘要
A new catalytic difluorohydration of beta-alkynyl ketones using NFSI as the fluorinating reagent has been established, diastereoselectively furnishing a range of structurally diverse difluoride 1,5-dicarbonyl products through C(sp(3))-H fluorination. Notably, the sterically encumbered t-butyl functionality located at the alpha-position of the carbonyl group of substrates 1 showed excellent diastereoselectivity (up to 499 : 1 dr). The reaction enabled multiple bond-forming events including two C(sp(3))-F formation through Ag-catalysis to provide a highly efficient and practical method toward difluoride 1,5-dicarbonyls, some of which were successfully converted into difluorinated isoquinolines.
- 出版日期2017-6-18
