- 212Pb/212Bi-EDTMP-Synthesis and biodistribution of a novel bone seeking alpha-emitting radiopharmaceutical
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At present, haematological toxicity is dose limiting in radionuclide therapy of bone metastases, and there is a need for radiopharmaceuticals with improved tumour/bone marrow dose ratios. Therefore, α-emitters e.g. 212Bi may be more suitable than β-emitters, because of the short range and high LET values of α-particIes. In this study, 212Bi and its mother nuclide 212Pb Were produced in an isotope generator by collecting gaseous 220Rn emanating from barium (228Th) stearate. The carrier-free 212Pb/212Bi Were bound to the chelating bone-seeking compound ethylene-diamine-tetra(methylene-phosphonic acid) (EDTMP) with 90% yield. The biodistribution in Balb/c mice was investigated by injecting 100 μl of a saline PBS buffer 0.020 M in EDTMP and 10 MBq/ml in 212Pb/212Bi. Mice were killed in groups of three at 0.5, 2, 13 and 24 h post-injection times. Both 212Pb EDTMP and 212Bi-EDTMP localised strongly in the skeleton, especially in the femur, at all time points measured, with the % of injected dose per gram (%ID/g) as high as 15 for 212Pb and 13 for 212Bi. All other organs investigated showed low uptake of both radionuclides, with the exception of the kidneys, for which a ratio femur/kidney of 1.5 for 212Bi 2 h Postinjection was observed. By comparison the ratio femur/blood was 20 for 212Bi 2 h Postinjection. The experiment indicates a potential for 212Pb/212Bi-EDTMP in targeted radiotherapy of osteoblastic bone lesions.
- Hassfjell,Hoff,Bruiand,Alstad
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- Structure-Dependent Dissolution and Restructuring of Calcite Surfaces by Organophosphonates
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Organophosphonates are well-known to strongly interact with the surfaces of various minerals, such as brucite, gypsum, and barite. In this work, we study the influence of six systematically varied organophosphonate molecules (tetraphosphonates and diphosphonates) on the dissolution process of the (10.4) surface of calcite. In order to pursue a systematic study, we have selected organophosphonates that exhibit similar structural features, but also systematic architectural differences. The effect of this class of additives on the dissolution process of the calcite (10.4) surface is evaluated using in situ dynamic atomic force microscopy. For all of the six organophosphonate derivatives, we observe a pronounced restructuring of the (10.4) cleavage plane of calcite, demonstrated by the formation of characteristically shaped etch pits. To elucidate their specific influence on the dissolution process of calcite (10.4), we vary systematically the number of functional end groups (two for the tetraphosphonates and one for the diphosphonates), the spacing between the functional ends through separating methylene groups (2, 6, and 12), as well as the pH of the solution (ranging from 2.6 up to 11.7). For each of the two groups of the organophosphonate derivatives, we observe the very same formation of etch pits (olive-shaped for the tetraphosphonate and triangular-shaped for the diphosphonate molecules), respectively. This finding indicates that the number of functional ends decisively determines the resulting calcite (10.4) surface morphology, whereas the size of the organophosphonate molecule within one group seems not to play any important role. For all of the molecules, the restructuring process of calcite (10.4) is qualitatively independent of the pH of the solution and, therefore, independent of the protonation/deprotonation states of the molecules. Our results reveal a general property of organophosphonate derivatives to induce surface restructuring of the calcite (10.4), which seems to be very robust against variations in both, different molecular structures and different protonation/deprotonation states.
- Nalbach, Martin,Moschona, Argyri,Demadis, Konstantinos D.,Klassen, Stefanie,Bechstein, Ralf,Kühnle, Angelika
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- METHOD FOR THE SYNTHESIS OF AMINOALKYLENEPHOSPHONIC ACID
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The present invention is related to a method for the synthesis of an aminoalkylenephosphonic acid or its phosphonate esters comprising the following steps: a) forming, in the presence of an aldehyde or ketone and an acid catalyst, a reaction mixture by mixing a compound comprising at least one HNR1R2 moiety or a salt thereof, with a compound having one or more P-O-P anhydride moieties, said moieties comprising one P atom at the oxidation state (+III) and one P atom at the oxidation state (+III) or (+V), wherein the ratio of moles of aldehyde or ketone to N-H moieties is 1 or more and wherein the ratio of N-H moieties to P-O-P anhydride moieties is 0.3 or more and, b) recovering the resulting aminoalkylenephosphonic acid comprising compound or its phosphonate esters.
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Paragraph 0084
(2014/02/15)
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- METHOD FOR THE SYNTHESIS OF ALPHA-AMINOALKYLENEPHOSPHONIC ACID
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The present invention is related to a new method for the synthesis of alpha-aminoalkylenephosphonic acid or its phosphonate esters comprising the steps of forming a reaction mixture by mixing a P-O-P anhydride moiety comprising compound, having one P-atom at the oxidation state (+111) and the other P-atom at the oxidation state (+111) or (+V), an aminoalkanecarboxylic acid and an acid catalyst, wherein said reaction mixture comprises an equivalent ratio of alpha-aminoalkylene carboxylic acid to P-O-P anhydride moieties of at least 0.2, and recovering the resulting alpha-aminoalkylene phosphonic acid compound or an ester thereof from the reaction mixture.
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Page/Page column 23
(2014/02/15)
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- Green synthesis of poly(aminomethylenephosphonic) acids
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The reaction of polyamines with phosphorous acid and formaldehyde in water under focused microwave irradiation provides a facile and rapid synthesis of poly(aminomethylenephosphonic) acids. Taylor & Francis Group, LLC.
- Villemin, Didier,Moreau, Bernard,Elbilali, Abdelghani,Didi, Mohamed-Amine,Kaid, Mhamed,Jaffres, Paul-Alain
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experimental part
p. 2511 - 2519
(2011/02/28)
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- METHOD FOR THE MANUFACTURE OF AMINO ALKYLENE PHOSPHONIC ACIDS
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A method for the manufacture of aminoalkylene phosphonic acids broadly is disclosed. In the essence, an amine corresponding to a specific formula is reacted in aqueous medium with phosphorous acid and formaldehyde to thereby yield a medium insoluble reaction product. The insoluble product formed i.e. the aminoalkylene phosphonic acid can be separated, optionally washed, and recovered. This process yields high purity and selectivity reaction products. The excess phosphonic acid can be recycled into the processing sequence.
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Page/Page column 14
(2010/12/26)
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- Process for the manufacture of alkylamino alkylene phosphonic acids
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A process for the manufacture of alkylamino alkylene phosphonic acids is disclosed. In detail, a specific phosphonate is reacted with an agent selected to yield an alkylamino moiety substituted by a radical selected from OH, OR', NH2, NHR', N(R')2, NH, N, S, S-S and SH in aqueous alkaline medium having a pH of 8 or higher at a temperature of 0°C or higher.
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Page/Page column 6; 7
(2008/12/06)
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- Process for the manufacture of aminopolyalkylene-phosphonic acid compounds
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A beneficial method for the manufacture of amino polyalkylene phosphonic acids, under substantial absence of hydrohalogenic acid, is disclosed. The method, in essence, is based on reacting narrowly defined ratios of phosphorous acid, an amine, a formaldehyde in presence of specific ranges of an acid catalyst having a pKa equal or inferior to 3.1. The inventive method is capable of yielding economically and quality operational/capacity advantages, in particular significantly reduced one-step cycle duration under exclusion of corrosion disadvantages and also is environmentally friendly without requiring, in that respect, anything more than nominal capital expenditures.
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Page/Page column 9; 13-14
(2008/06/13)
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- NOVEL UNSYMMETRICAL N,N-BIS(METHYLENE)BIPHOSPHONIC ACIDS OF α,ω-DIAMINES. PREPARATION AND CHARACTERIZATION OF BIS(METHYLENE)>-BIPHOSPHONIC ACID AND BIS(METHYLENE)>-BIPHOSPHONIC ACID
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Reaction of ethylenediamine with phosphorous acid and formaldehyde in molar ratio 1:2:2 gives bis(methylene)>biphosphonic acid (2a) as the major product.Similarly, reaction of hexamethylenediamine with phosphorous acid and formaldehyde in molar ratio 1:2:2 yields bis(methylene)>biphosphonic acid (2b) which is isolated either as bis(methylene>biphosphonic acid (3b) or as bis(methylene)>biphosphonic acid (4b).Removal of the carbobenzoxy group with HBr 3b or the benzoyl group with HCl from 4b gives pure bis(methylene)>biphosphonic acid (2b).All compounds were characterized by 13C NMR, 31P NMR and elemental analysis.
- Redmore, Derek,Dhawan, Balram
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p. 233 - 238
(2007/10/02)
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