15049-85-1

Usage

Uses

Used in Pharmaceutical Industry:
(1-aminoethylidene)bisphosphonic acid is used as a therapeutic agent for the treatment of osteoporosis and other bone-related diseases. Its application is based on its ability to slow down bone breakdown and increase bone density, which helps prevent fractures and maintain bone strength in patients.
Used in Postmenopausal Women's Health:
(1-aminoethylidene)bisphosphonic acid is used as a preventive measure for hip, spine, and other fractures in postmenopausal women with osteoporosis. Its application is due to its effectiveness in reducing the risk of such fractures, making it an important medication for the management of bone health in this demographic.

InChI:InChI=1/C2H9NO6P2/c1-2(3,10(4,5)6)11(7,8)9/h3H2,1H3,(H2,4,5,6)(H2,7,8,9)

Upstream product

• 75-05-8 acetonitrile 
• 762-04-9 phosphonic acid diethyl ester 
• 60-35-5 acetamide 
• 1605320-74-8 tetrakis(trimethylsilyl) (1-aminoethane-1,1-diyl) bisphosphonate 

Downstream Products

• 13598-36-2 phosphonic Acid 

Relevant academic research and scientific papers

Synthesis and biological evaluation of 1-amino-1,1-bisphosphonates derived from fatty acids against Trypanosoma cruzi targeting farnesyl pyrophosphate synthase

We have investigated the effect of a series of 1-amino-1,1-bisphosphonates derived from fatty acids against proliferation of the clinically more relevant form of Trypanosoma cruzi, the causative agent of American trypanosomiasis (Chagas' disease). Some of these drugs were potent inhibitors against the intracellular form of the parasite, exhibiting IC50 values at low micromolar level. Cellular activity was associated with the inhibition of enzymatic activity of T. cruzi farnesyl pyrophosphate synthase. As bisphosphonate-containing drugs are FDA-approved for the treatment of bone resorption disorders, their potential innocuousness makes them good candidates to control tropical diseases.

1-acetamido-ethylidene-1,1-bisphosphonate and preparation method and application thereof

The invention discloses a 1-acetamido-ethylidene-1,1-bisphosphonate, and particularly discloses a 1-acetamido-ethylidene-1,1-calcium diphosphate. A structural formula of the 1-acetamido-ethylidene-1,1-bisphosphonate is as shown in a formula (I). The invention further discloses a preparation method of the compound in the formula (I). The compound in the formula (I) has an anti-radiation effect, especially has an excellent discharge-facilitating effect on strontium, is stable in property and good in water solubility, and can be used as a high-efficiency and low-toxicity discharge-facilitating drug for pollution in radioactive strontium.

Synthesis of (aminomethylene)bisphosphonic acid derivatives

Amino derivatives of methylenebisphosphonic acids were synthesized by phosphorylation of formamide, nitriles or hydrochlorides of alkyl imidates with H3PO3—PCl3—(Me3Si)2NH.

Synthesis of substituted N-formylaminomethylenediphosphonates and their derivatives

The convenient methods for the synthesis of new trimethylsilyl esters of aminomethylenediphosphonic acids are elaborated. The new substituted N-formylaminomethylenediphosphonates are obtained via the interaction of trimethylsilyl esters of methylenediphosphonic acids with a mixture of triethyl orthoformate and ethanol. Also boron trifluoride-diethyl etherate as an effective catalyst is used for the interaction of hydrochlorides of ethoxymethylene imines with diethyl trimethylsilyl phosphite. The corresponding aminomethylenediphosphonic acids are presented.

Synthesis of the new types of N-unsubstituted aminomethylenebisorganophosphorus acids and their derivatives

The interaction of trimethylsilyl esters of trivalent organophosphorus acids containing PH and POSiMe3 groups with hydrochlorides of ethoxymethylene imines is a convenient method for the synthesis of new trimethylsilyl esters of N-unsubstituted aminomethylenebisorganophosphorus acids with three and four coordinated phosphorus. Also trimethylsilyl trifluoromethanesulfonate as effective catalyst is used for the similar interaction of hydrochlorides of ethoxymethylene imines with tris(trimethylsilyl)phosphite. The corresponding bisorganophosphorus acids and their derivatives are presented.

Synthesis of new types of aminomethylenediphosphorus-containing acids and their derivatives

Convenient methods for synthesis of various aminomethylenediphosphorus-containing acids and their derivatives starting from available trimethylsilyl esters of hypophosphorous and phosphorous acids, ethoxymethyleneimine hydrochlorides, and N-substituted formamides have been proposed. Selected properties of the obtained compounds have been examined.

Non-hydrolysable analogues of inorganic pyrophosphate as inhibitors of hepatitis C virus RNA-dependent RNA-polymerase

Inorganic pyrophosphate (PPi) is the product of the polymerization reaction catalyzed by DNA-and RNA-polymerases. A number of novel non-hydrolsable PPi analogues was synthesized; some of them inhibited the polymerization reaction catalyzed by hepatitis C virus RNA-dependent RNA-polymerase (NS5B). A new pharmacophore based on a non-hydrolysable methylenediphosphonate backbone has been developed. The structure-activity relationship analysis of 12 bisphosphonates is presented and the structural features crucial for NS5B polymerase activity inhibition are stated. Pleiades Publishing, Ltd., 2012.

Copper(II) complexes of organophoshonic acids-a comparative study

Polynuclear copper(II) derivatives of 1-hydroxyethylidenediphosphonic acid (HEDP), 1-aminoethylidenediphosphonic acid (AEDP, H4L), α- aminobenzylidene diphosphonic acid (ABDP, H4L), 1-amino-2-carboxyethane- 1,1-diphosphonic acid (ACEDP, H5L), 1,3 diaminopropane-1,1,3,3- tetraphosphonic acid (DAPTP, H8L), Ethylenediamine-N,N'-bis (dimethylmethylenephosphonic) acid (EDBDMPO, H4L), o-phenylene-diamine-N,N'-bis (dimethylmethylenephosphonic) acid (PDBDMPO, H4L), diethylene triamine -N,N,N',N',N''N"-penta (methylene phosphonic) acid (DETAPMPO, H 10L) and diethylene triamine -N,N''-bis (dimethyl methylene phosphonic) acid (DETBDMPO, H4L) have been prepared in aqueous medium. The general formula of derivatives from elemental analysis was found to be Cu2L.XH2O (in case of AEDP, ABDP, EDBDMPO, PDBDMPO, DETBDMPO), Cu 5L2.XH2O (in case of ACEDP) Cu4L.XH2O, Cu2 H4L. XH2O (in case of DAPTP) and Cu5L.XH2O (in case of DETAPMPO). The electronic spectra have shown them to be six coordinated with slight distortion from octahedral geometry. Antiferromagnetism was inferred from magnetic moment data. Infrared spectral studies were carried out to determine coordination sites. EPR (Electron Paramagnetic Resonance) spectra that supports the presence of tetragonal distortion and antiferromagnetic behaviour, have also been studied.