This chapter deals with the synthesis of α-organyl-substituted
methylenebisphosphonates and focuses on compounds not having the heteroatomic
substituents at the geminal carbon. We present different methodologies on the basis of
the reactivity of monophosphonate and methylene 1,1-bisphosphonate systems
including the Michaelis-Arbuzov and Michaelis-Becker reactions, substitutions,
Michael additions, cycloaddition, as well as more specific approaches. Together with
the synthetic methods, the biomedical application of the compounds is also described.
Keywords: Alkenylidene-1, 1-Bisphosphonates, Alkylation, Anti-Inflammatory
Properties, Anti-Resorption Agents, Antitumor, Asymmetric Synthesis, Bone
Targeting, Bisphosphonates, Bisphosphonate Conjugates, Cycloaddition, Enzyme
Inhibitors, Michaelis-Arbuzov Reaction, Michael Additions, Phosphorylation,
Pyrophosphate Bioisosteres, Phosphate Mimics, Phosphonate Carbanions, Three-
Component Reactions.
