Solventless synthesis of acyl phosphonamidates, precursors to masked bisphosphonatesElectronic supplementary information (ESI) available. See DOI: 10.1039/c5cc03549j

• Main Authors: Crossey, Kerri, Migaud, Marie E
• Format: Journal Article
• Language: English
• Published: 25.06.2015
• ISSN: 1359-7345; 1364-548X
• DOI: 10.1039/c5cc03549j

A series of acyl phosphonamidates, the synthetic precursors to bisphosphonates, have been readily prepared from phosphoramidite type reagents and a range of acid chlorides. These reactions were performed using solventless conditions, where purification was easily achieved using column chromatography with yields ranging from 71-90%. Furthermore, we have demonstrated that these acyl phosphonamidates could be used for the preparation of unsymmetrical bisphosphonates, which do date are scarcely reported in the literature. A series of acyl phosphonamidates, the synthetic precursors to bisphosphonates, have been readily prepared from phosphoramidite type reagents and a range of acid chlorides.