title: Solventless synthesis of acyl phosphonamidates, precursors to masked bisphosphonates.
abstract: 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.
authors.affiliation: John King Laboratory, School of Pharmacy, Queen's University Belfast, 97 Lisburn Road, Belfast, BT9 7BL, UK. m.migaud@qub.ac.uk.
authors.forename: Kerri
authors.initials: K
authors.lastname: Crossey
authors.forename: Marie E
authors.initials: ME
authors.lastname: Migaud
mesh_terms: D000577:Amides / Q000138:chemical synthesis* / Q000737:chemistry; D015394:Molecular Structure; D009946:Organothiophosphorus Compounds / Q000138:chemical synthesis* / Q000737:chemistry; D010756:Phosphoric Acids / Q000138:chemical synthesis* / Q000737:chemistry
chemical_list: D000577:Amides; D009946:Organothiophosphorus Compounds; D010756:Phosphoric Acids; C011067:phosphoramidic acid