Modular Synthesis of Polycarbonyl Compounds via Regioselective Hydration of Oxo-Alkynes

A novel protocol has been developed for the modular synthesis of polycarbonyl compounds by catalytic hydration of 1,3-diketone-tethered alkynes. The hydration process exhibits good regioselectivity and high yields at room temperature, avoiding the use of strong acids and noble metals and the requirement for elevated temperatures. Mechanistic insights suggest that the hydration proceeds through a concerted process of alkyne protonation and remote carbonyl participation. This approach provides direct access to tandem heterocycle dyads and triads.