Diastereoselective synthesis of α,α′-disubstituted β-ketophosphonates derivatives as building blocks for automated syntheses

A convenient and efficient synthesis of α,α′-disubstituted β-ketophosphonic derivatives in good to excellent de’s and yields has been achieved by α-acylation followed by diastereoselective α-alkylation of chiral 5-membered cyclic phosphonamidates.

Graphical abstractA convenient and efficient synthesis of α,α′-disubstituted β-ketophosphonic derivatives in good to excellent de’s and yields has been achieved by α-acylation followed by diastereoselective α-alkylation of chiral 5-membered cyclic phosphonamidates.Figure optionsDownload full-size imageDownload as PowerPoint slide