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Beilstein J. Org. Chem. 2015, 11, 1425–1433, doi:10.3762/bjoc.11.154
Graphical Abstract
Figure 1: A sampling of propargylamine-derived triazoles with therapeutic effects includes alpha-tetrasubstit...
Figure 2: A tetrasubstituted carbon bearing an amine (red) can provide 100-fold increase in activity compared...
Scheme 1: KA2 coupling followed by tandem silyl deprotection and triazole formation.
Scheme 2: Silyl deprotection/click conditions applied to tert-butylacetylene. An identical yield is observed ...
Scheme 3: High overall yield of 1,2,3-triazole fully-substituted at the 4-position.