Microwave-assisted synthesis of (aminomethylene)bisphosphine oxides and (aminomethylene)bisphosphonates by a three-component condensation

• Erika Bálint,
• Ádám Tajti,
• Anna Dzielak,
• Gerhard Hägele and
• György Keglevich

Beilstein J. Org. Chem. 2016, 12, 1493–1502, doi:10.3762/bjoc.12.146

• Chemistry, Heinrich-Heine-University Düsseldorf, 40225 Düsseldorf, Germany 10.3762/bjoc.12.146 Abstract A practical method was elaborated for the synthesis of (aminomethylene)bisphosphine oxides comprising the catalyst- and solvent-free microwave-assisted three-component condensation of primary amines

• together with a few by-products could also be identified. Keywords: (aminomethylene)bisphosphine oxides; (aminomethylene)bisphosphonates; microwave; three-component condensation; Introduction Substituted (hydroxymethylene)bisphosphonic acid derivatives form an important group of drugs used in the

• ]. (Aminomethylene)bisphosphonates can also be obtained starting from amides, triethyl phosphite and phosphorus oxychloride (Scheme 3a) [37], or in the reaction of amines with diazophosphonate in the presence of a rhodium catalyst (Scheme 3b) [38]. (Aminomethylene)bisphosphine oxides are analogous to (aminomethylene