Abstract

AbstractAn efficient synthesis of functionalized alkynyl phosphine oxides is described. The current approach is based on the activation of the phosphorus−hydrogen bond (P−H bond) of a secondary phosphine oxide. After the deprotonation step using n‐butyllithium, the in‐situ generated LiP(O)RR’ undergoes further condensation with a wide variety of electrophiles, and without a cyclisation step into the alkyne as a side reaction. In particular, the addition to aldehydes proceeds quickly and gives access to α‐hydroxy phosphine oxides, with a diastereoselectivity rate up to 80/20.

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