Catalytic asymmetric synthesis of stable oxetenes via Lewis acid-promoted [2+2] cycloaddition.

摘要: A highly enantioselective and atom-economical [2 + 2] cycloaddition of various alkynes with trifluoropyruvate using a dicationic (S)-BINAP–Pd catalyst has been established. This is the first synthesis stable oxetene derivatives, whose structure clarified by X-ray analysis. catalytic process offers practical synthetic method for derivatives (catalyst loading: up to 0.1 mol %), which can serve as novel chiral building blocks pharmaceuticals agrochemicals also be transformed into variety enantiomerically enriched CF3-substituted compounds high stereoselectivity.