Abstract
A facile and efficient method for the synthesis of trifluoromethylated carbinols has
been developed from imidazo[1,2-a ]pyridines and trifluoroacetaldehyde. The direct C(sp2 )–H hydroxytrifluoromethylation is successfully implemented at room temperature using
HFIP as solvent through dehydrative cross-coupling process, which displays a broad
substrate scope and functional group tolerance. Furthermore, gram-scale and synthetic
transformation experiments have also been demonstrated, which indicate its potential
applicable values in organic synthesis. This green protocol features operational simplicity,
atom economy, mild reaction conditions (e.g., at room temperature, transition-metal-
and oxidant-free, without inert gas protection), wide substrate scope, and excellent
practicality.
Key words imidazo[1,2-
a ]pyridines - trifluoromethylated carbinols - dehydrative cross-coupling - HFIP - metal-free
