Journal
ORGANIC LETTERS
Volume 19, Issue 11, Pages 2881-2884Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.7b01116
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Funding
- Chinese University of Hong Kong Start-up Fund
- Faculty Strategic Development Funding
- Direct Grant for Research [4053199]
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We herein describe a. Cu(I)-catalyzed interrupted click reaction, using (trifluoromethyl)trimethylsilane (TMSCF3) as a nucleophilic CF3 source, to synthesize 5-trifluoromethyl 1,2,3-triazoles in one step from readily available terminal alkynes, and azides. The reaction shows complete regioselectivity, broad substrate scope, and good functional group tolerability. The application of the reaction had, been demonstrated in the synthesis of, a trifluoromethylated analog of antiepileptic drug rufinamide.
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