Abstract
The general method for the tandem phosphination-decarboxylation-oxidation of alkynyl acids under aerobic conditions has been developed. In the presence of CuSO4·5H2O and TBHP, the reactions provide a novel access to β-ketophosphine oxides in good to excellent yields. This transformation allows the direct formation of a P-C bond and the construction of a keto group in one reaction.
Highlights
The general method for the tandem phosphination–decarboxylation– oxidation of alkynyl acids under aerobic conditions has been developed
In the presence of CuSO4Á5H2O and TBHP, the reactions provide a novel access to b-ketophosphine oxides in good to excellent yields
This transformation allows the direct formation of a P–C bond and the construction of a keto group in one reaction
Summary
The general method for the tandem phosphination–decarboxylation– oxidation of alkynyl acids under aerobic conditions has been developed. In the presence of CuSO4Á5H2O and TBHP, the reactions provide a novel access to b-ketophosphine oxides in good to excellent yields. When a mixture of 1a (0.2 mmol), 2a (0.8 mmol), CuSO4Á5H2O (0.02 mmol) and NH3ÁH2O (25%, 0.25 mL) in MeCN was heated to 60 1C in air for 2 h, the desired product 3a was obtained in 43% yield (Table 1, entry 1).
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