Abstract

A thorough study on copper-free Sonogashira cross-couplings in water was carried out using the palladacycle, [{Pd(μ-Cl){κ2-P,C-P(iPr)2(OC6H3-2-Ph)}}2] as pre-catalyst with different bases and palladium concentrations. The highly active pre-catalyst imparts good to near quantitative yields using a concentration of 0.25mol% at 40°C. This broadly applicable protocol exhibits high tolerance of functional groups and substitution patterns.

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