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A new route to α-alkyl-α-fluoromethylenebisphosphonates†
Petr Beier,Stanislav Opekar,Mikhail Zibinsky,Inessa Bychinskaya,G. K. Surya Prakash
Organic & Biomolecular Chemistry Pub Date : 04/28/2011 00:00:00 , DOI:10.1039/C1OB05095H
Abstract

A new route to α-alkyl-α-fluoromethylenebisphosphonates, 2 has been developed starting from commercially available tetraethyl fluoromethylenebisphosphonate (1), and alkyl halides using either caesium carbonate in DMF or sodium dimsyl. De-esterification of 2 provided biologically important α-alkyl-α-fluoromethylenebisphosphonic acid, 3, while alkoxide–induced carbon–phosphorus bond cleavage of 2 gave α-fluorophosphonates, 4, which are useful synthons in organic synthesis.

Graphical abstract: A new route to α-alkyl-α-fluoromethylenebisphosphonates
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