3794-83-0Relevant articles and documents
One-pot synthesis of phosphinylphosphonate derivatives and their anti-tumor evaluations
Deschamp, Julia,Dussart-Gautheret, Jade,Lecouvey, Marc,Legigan, Thibaut,Migianu-Griffoni, Evelyne,Monteil, Maelle
, (2021/12/24)
This paper reports on the synthesis of new hydroxymethylene-(phosphinyl)phosphonates (HMPPs). A methodology has been developed to propose an optimized one-pot procedure without any intermediate purifications. Various aliphatic and (hetero)aromatic HMPPs were synthesized in good to excellent yields (53–98%) and the influence of electron withdrawing/donating group substitution on aromatic substrates was studied. In addition, the one-pot synthesis of HMPP was monitored by31P NMR spectroscopy, allowing effective control of the end of the reaction and identification of all phosphorylated intermediate species, which enabled us to propose a reaction mechanism. Optimized experimental conditions were applied to the preparation of biological relevant aminoalkyl-HMPPs. A preliminary study of the complexation to hydroxyapatite (bone matrix) was carried out in order to verify its lower affinity towards bone compared to bisphosphonate molecules. Moreover, in vitro anti-tumor activity study revealed encouraging antiproliferative activities on three human cancer cell lines (breast, pancreas and lung).
Optimized synthesis of etidronate
Kovacs, Rita,Nagy, David Illes,Gruen, Alajos,Balogh, Gyoergy Tibor,Garadnay, Sandor,Greiner, Istvan,Keglevich, Gyoergy
, p. 733 - 737 (2013/12/04)
The synthesis of Etidronate (as the disodium salt) by the reaction of acetic acid with phosphorus trichloride/phosphorus acid in methanesulfonic acid was studied and optimized. We showed that it is enough to use 3.2 equivalents of the phosphorus trichlori
Aminohydroxypropane esters of hydroxyethylidenebisphosphoric acid.
Chuiko, Alexey,Philonenko, Ludmila,Borisevich, Anatoly,Lozinsky, Miron
, p. 66 (2007/10/03)
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