The synthesis of the disodium salt of fenidronate by the reaction of benzoic acid with phosphorus trichloride and phosphorous acid in methanesulfonic acid was investigated and optimized. It was enough to use 3.2 equivalents of phosphorus trichloride and t
Gruen, Alajos,Kovacs, Rita,Nagy, David Illes,Garadnay, Sandor,Greiner, Istvan,Keglevich, Gyoergy
Phenyl-, benzyl-, and unsymmetrical hydroxy-methylenebisphosphonates as dronic acid ester analogues from α-oxophosphonates by microwave-assisted syntheses
The microwave (MW)-assisted addition of dialkyl phosphites to α-oxophosphonates was investigated and optimized under solventless conditions to provide the phenyl- and benzyl-hydroxy-methylenebisphosphonates efficiently by suppressing the rearrangement sid
Synthesis of α-hydroxy-methylenebisphos-phonates by the microwave-assisted reaction of α-oxophosphonates and dialkyl phosphites under solvent ess conditions
The synthesis of hydroxy-methyl-enebisphosphonates (2a-c) by the addition of dialkyl phosphite to the carbonyl group of the corresponding α-oxophosphonate (1a-c) was studied under microwave irradiation (MW) and solventless conditions in the presence of di
A one pot synthesis of symmetric methyl, benzyl hydroxy bisphosphonic esters can be obtained, without the use of a dialkylphosphite by introducing a protic reagent which removes the usual α-ketophosphonate step.
Benech,El Manouni,Leroux
p. 295 - 298
(2007/10/03)
α CETOPHOSPHONATES ET ESTERS CYCLIQUES D'HYDROXYMETHYLENES DIPHOSPHONATES SYNTHESES, STRUCTURES ET HYDROLYSE
Synthesis of symmetrical diesters derived from hydroxy methylene diphosphonic acids 1 to 8 is described either in one step or via the corresponding α ketophosphonate 1a to 8a.Study of the diphosphonates (1 to 6) -> phosphate-phosphonates (1b to 6b) isomerization has been realized.Results related to peculiar cases in connection with nonsymmetrical esters 10, 11, 17 and study of the hydrolysis reaction of diphosphonates are presented.
Tromelin, Anne,El Manouni, Driss,Burgada, R.
p. 301 - 312
(2007/10/02)
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