Journal
ORGANIC LETTERS
Volume 21, Issue 1, Pages 65-69Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.8b03505
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Funding
- Lundbeck Foundation [R250-2017-1292]
- Technical University of Denmark
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A copper-catalyzed route to alpha-substituted, primary benzylamines by C-H functionalization of alkylarenes is described. The method directly affords the amine hydrochloride salt. Catalyst loadings down to 0.1 mol % in combination with scalability, insensitivity to air and moisture, and no need for column chromatography makes the procedure highly practical. The facile synthesis of the racemate of a blockbuster drug highlights the relevance for the development of pharmaceuticals. Preliminary mechanistic data are also included.
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