- Synthesis of ω-phthalimidoalkylphosphonates
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A series of carbon chain growing ω-phthalimidoalkylphosphonates was prepared from simple and easy available raw materials by twostep reaction. The yields can reach 58 %-64 %. Their structures are confirmed by 1H NMR correctly.
- Zhou, Liang
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experimental part
p. 4821 - 4822
(2012/08/14)
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- Studies on the synthesis of a chiral salen Mn (III) complex immobilised onto zirconium aminophosphonates and catalytic asymmetric epoxidation of α-methylstyrene
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A chiral salen Mn (III) complex has been immobilised onto zirconium aminophosphonates by axial coordination with different linkage arm lengths (CH2)n (n = 2-6), to give a series of heterogeneous catalysts. The catalysts exhibited good to excellent catalytic efficiency in the asymmetric epoxidation of α-methylstyrene. One heterogeneous catalyst, with n = 6, gave higher catalytic properties than the original chiral salen Mn (III) complex in the NaClO/PPNO system. It can be easily recovered and reused several times without significant loss of activity.
- Zhou, Liang
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p. 512 - 515
(2012/10/29)
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- Synthesis and characterization of aminophosphonates zirconium as new mesoporous materials
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A serial of aminophosphonates zirconium with the different arm lengths of -(CH2)n- organic chains (n=2-6) was synthesized for the first time. These compounds are characterized by FT-IR, SEM, TEM, TG and nitrogen adsorption-desorption. And based on the experimental data, these materials not only have layer structure mesoporous and good thermal stability such as zirconium phosphate, but also can be adjusted the layer distance, pore size and pore volume. So aminophosphonates zirconium posses special excellent properties and will have potential prospect applications.
- Zhou, Liang
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experimental part
p. 1320 - 1326
(2012/05/21)
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- COMPOUNDS AND METHODS FOR INHIBITING NHE-MEDIATED ANTIPORT IN THE TREATMENT OF DISORDERS ASSOCIATED WITH FLUID RETENTION OR SALT OVERLOAD AND GASTROINTESTINAL TRACT DISORDERS
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The present disclosure is directed to corn- pounds and methods for the treatment of disorders associated with fluid retention or salt overload, such as heart failure (in particular, congestive heart failure), chronic kidney disease, end-stage renal disease, liver disease, and peroxisome proliferator-activated receptor (PPAR) gamma agonist-induced fluid retention. The present disclosure is also directed to compounds and methods for the treatment of hypertension. The present disclosure is also directed to compounds and methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders. The methods generally comprise administering to a mammal in need thereof a pharmaceutically effective amount of a compound, or a pharmaceutical composition comprising such a compound, that is designed to be substantially active in the gastrointestinal (GI) tract to inhibit NHE-mediated antiport of sodium ions and hydrogen ions therein. More particularly, the method comprises administering to a mammal in need thereof a pharmaceutically effective amount of a compound, or a pharmaceutical composition comprising such a compound, that inhibits NHE-3, -2 and/ or -8 mediated antiport of sodium and/or hydrogen ions in the GI tract and is designed to be substantially impermeable to the layer of epithelial cells, or more specifically the epithelium of the GI tract. As a result of the compound being substantially impermeable, it is not absorbed and is thus essentially systemically non-bioavailable, so as to limit the exposure of other internal organs (e.g., liver, heart, brain, etc.) thereto. The present disclosure is still further directed to a method wherein a mammal is administered such a compound with a fluid-absorbing polymer, such that the combination acts as described above and further provides the ability to sequester fluid and/or salt present in the GI tract
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Page/Page column 148
(2010/08/04)
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- A general synthesis of ethyl 4-aminophenyl and ethyl 4-[amino(hydroxyimino)methyl]phenyl phosphonates
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Diethyl phosphonates were conveniently converted into ethyl 4-aminophenyl and ethyl 4-[amino(hydroxyimino)methyl]phenyl phosphonates as potentially useful intermediates for the preparation of functionalized phenyl phosphonates.
- Gobec, Stanislav,?trancar, Katja,Urleb, Uro?
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p. 167 - 170
(2007/10/03)
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- Facile ring-opening reactions of phthalimides as a new strategy to synthesize amide-functionalized phosphonates, primary phosphines, and bisphosphines
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The nucleophile-assisted ring-opening reaction of phthalimides 1 has been studied. The reaction of phthalimides 1 with 0.5 equiv of hydrazine produced the novel bisphosphonates 2 in near quantitative yields whereas with 10-fold excess of hydrazine, diethyl aminoalkylphosphonates 3 was formed in 75% yields. The reaction of phthalimide 1b with 3-(aminopropyl)phosphine resulted in a novel compound 4a containing a P(III) hydride and a P(V) phosphonate within the same molecule. In addition, the reaction of 1b with 2- aminoethanol and 2-aminoethanethiol resulted in the formation of new phosphonates 4b,c. The reaction of bisphosphonates 2 with LiAlH4 in THF at 0 °C selectively reduced the phosphonate groups producing corresponding air- stable primary bisphosphines 6 in 80% yields. Further, the formylation of bisphosphines 6 under very mild conditions using 37% aqueous formaldehyde produced the corresponding novel water-soluble bisphosphine chelating agents 7 in near quantitative yields. All the new compounds have been characterized by 1H, 13C, 31P NMR, IR spectroscopy and mass spectrometry.
- Gali, Hariprasad,Prabhu, Kandikere R.,Karra, Srinivasa R.,Katti, Kattesh V.
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p. 676 - 680
(2007/10/03)
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- Synthesis of ω-phthalimidoalkylphosphonates
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Diethyl phthalimidoalkylphosphonates were synthesized by the reaction of diethyl bromoalkylphosphonates with N-(tert-butyldimethylsilyl)phthalimide in the presence of tetrabutylammonium fluoride.
- Chun,Park,Oh,Hong,Kim
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p. 909 - 910
(2007/10/02)
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- ORGANOPHOSPHORUS COMPOUNDS AS POTENTIAL FUNGICIDES. PART II. AMINOALKANE-, GUANIDINOALKANE-, AND THIOUREIDOALKANE-PHOSPHONIC ACIDS: PREPARATION, SPECTROSCOPY, AND FUNGICIDAL ACTIVITY
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A range of α-amino-, ω-amino-, α-guanidino-, and ω-guanidinoalkanephosphonic acids has been prepared for the purpose of studying their spectroscopic features and fungicidal activity.In addition, α-thioureido-octanephosphonic acid and thioureylene-1,1-bis(1-octanephosphonic acid) were isolated during the preparation of α-guanidino-octanephosphonic acid. 31P, 1H, and 13C nmr spectral data which were obtained for solutions of the amino- and guanidino-compounds in D2O or D2O/D2SO4, and for the thioureido compounds in DMSO-d6, are discussed together with previouslyreported data for the aminophosphonic types.FAB mass spectrometry generally gives strong pseudomolecular ions + for the zwitterionic amino- and guanidino-compounds with relatively simple fragmentations.Fungicidal activity of the α-aminophosphonic acids was found to be greater than for the ω-amino compounds, with maximum activity at a chain length of three carbon atoms when used as a seed dressing for the control of Drechslera spp.Moderately good activity was shown by the thioureido compounds against a number of fungal organisms in vitro but the guanidino-compounds exhibited low activity.Key words: Organophosphorus; fungicides; aminophosphonic acids; guanidinophosphonic acids; NMR spectroscopy; FAB mass spectroscopy.
- Cameron, David G.,Hudson, Harry R.,Pianka, Max
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- Syntheses of Phosphonic- and Phosphinic Analogues of Pantothenic Acid Ethyl Ester and of the Phosphonic Analogue of Pantetheine
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The replacement of amino acids in peptides by phosphono-analogous (aminoalkyl)phosphonic acids 1, (2-aminoethyl)phosphonic acid (2) and substituted derivatives has been an important aspect of peptides research in the last years.In pantothenic acid (3), there is a peptide linkage between (2R)-2,4-dihydroxy-3,3-dimethylbutyric acid and the amino group of β-alanine, and in pantetheine (4), there is a second peptide linkage between the β-alanine and cysteamine.The synthesis of phosphono and phosphino analogues of pantothenic acid ethyl ester, where the β-alanine is replaced by the diethyl ester of (2-aminoethyl)phosphonic acid and the ethyl ester of (2-aminoethyl)methylphosphonic acid, respectively, and the syntheses of the phosphono analogue of pantetheine, where the β-alanine is replaced by (2-aminoethyl)phosphonic acid, are described.
- Neidlein, Richard,Greulich, Peter
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p. 2545 - 2552
(2007/10/02)
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- Synthesis of Peptide Analogues Containing (2-Aminoethyl)phosphonic Acid (Ciliatine)
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Di- and tripeptide analogues containing (2-aminoethyl)phosphonic acid , which has been discovered in a wide variety of living organisms, were prepared.As starting materials for incorporating the amino phosphonic acid into a peptide chain, the N-phthalylated diethyl ester and the N-carbobenzyloxylated monoalkyl ester were used.A phosphonamide bond between the amino phosphonic acid unit and amino acid unit was formed by reaction of Pht-Aep(OEt)Cl with amino acid ethyl ester or coupling reaction between Cbz-Aep(OR)(OH) and amino acid ethyl ester using diphenylphosphoryl azide-triethylamine as a condensing agent.Removal of the protecting groups was studied in connection with the acid-labile phosphonamide bond in the abnormal peptides.
- Yamauchi, Kiyoshi,Ohtsuki, Souichi,Kinoshita, Masayoshi
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p. 1158 - 1163
(2007/10/02)
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