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)bisphosphineoxides 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)bisphosphineoxides; (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)bisphosphineoxides are analogous to (aminomethylene
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Graphical Abstract
Scheme 1:
Proposed routes for the three-component condensation [7].