A new synthetic method characterized by low environmental impact for the synthesis of a wide range of gem-bisphosphonates bearing aryl substituents in β position as potential anti-resorption species to contrast osteoporosis is reported. The pivotal role played by water ensures higher yields compared to the organic medium in the rhodium-catalyzed 1,4-conjugate addition of arylboronic acids to vinylidenebisphosphonate tetraethylester, as well as easy product isolation
Water Enhanced Synthesis of gem-Bisphosphonates via Rh(I) Mediated 1,4-Conjugate Addition of Aryl Boronic Acids to Vinilydenbisphosphonate Esters
SCARSO, Alessandro;CHIMINAZZO, ANDREA;SPERNI, Laura;STRUKUL, Giorgio
2013-01-01
Abstract
A new synthetic method characterized by low environmental impact for the synthesis of a wide range of gem-bisphosphonates bearing aryl substituents in β position as potential anti-resorption species to contrast osteoporosis is reported. The pivotal role played by water ensures higher yields compared to the organic medium in the rhodium-catalyzed 1,4-conjugate addition of arylboronic acids to vinylidenebisphosphonate tetraethylester, as well as easy product isolation
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