Copper powder-catalyzed α-alkynylation of secondary alcohols via an isodesmic reaction was established. The synergistic interaction between copper powder and 1,10-phenanthroline was identified as the pivotal factor in significantly boosting the activity of the reaction. This α-alkynylation of secondary alcohols provides a step-economic procedure for preparing CF3-substituted propargylic alcohols. This reaction proceeds under open-air conditions, exhibiting a broad substrate scope and excellent compatibility with the late-stage modification of bioactive molecules.
Lin et al. (Tue,) studied this question.