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A general synthesis of ethyl 4-aminophenyl and ethyl 4-[amino(hydroxyimino)methyl]phenyl phosphonates

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.

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Cationic lipids

The present invention discloses cationic lipids useful for making lipid aggregates for delivery of macromolecules and other compounds into cells. They are especially useful for the DNA-dependent transformation of cells. Also disclosed are lipids useful both for the delivery of macromolecules and also useful as intermediates for making other such lipids.

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Discovery of 8-Boc-2,8-Diazaspiro[4.5]decane

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STRUCTURE OF THE PRODUCT FROM THE RAECTION OF 2-BROMOETHYLPHTHALIMIDE WITH POTASSIUM HYDROXIDE

The reaction of 2-bromoethylphthalimide with potassium hydroxide leads to the formation of 2-(2-carboxyphenyl)oxazoline and not the cyclic phthalimidic ester as indicated in the literature.

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Awesome Chemistry Experiments For 8-Boc-2,8-Diazaspiro[4.5]decane

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A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, Computed Properties of C13H24N2O2, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 236406-39-6, Name is 8-Boc-2,8-Diazaspiro[4.5]decane, molecular formula is C13H24N2O2. In a Article, authors is Ferroni£¬once mentioned of 236406-39-6

Synthesis and platelet aggregation inhibitory effects of N-[(1H-pyrazol-1-yl)alkyl]benzoylamides

A series of N-[(1H-pyrazol-1-yl)alkyl]benzoylamides was synthesized and tested in vitro for their inhibitory effects on adenosine diphosphate-, collagen-, arachidonic acid- and thrombin-induced aggregation of human platelets. Among them, N-[(1H-pyrazol-1-yl)butyl]benzoylamide (Ve) was found to have the most potent inhibitory activity. The structure-activity relationships are reported. The biological activity of the title compounds is reported in parallel with that of a known inhibitor of thromboxane A2 synthetase.

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Synthesis of new omega-amino- and omega-azidoalkyl carboranes

Novel carboranyl amines [7-NH2(CH2) nS-7,8-C2B9H11]- were synthesized by alkylation of 1-mercapto-ortho-carborane with omega-bromoalkylphthalimides followed by removal of the protecting group with hydrazine. closo-Carboranyl azides 1-N3(CH2) nS-1,2-C2B10H11 were prepared by the reaction of the corresponding carboranyl alcohol/iodide with sodium azide and converted to the water soluble nido-form [7-N3(CH2) nS-7,8-C2B9H11]- with ammonium formate in refluxing methanol.

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A new application about 8-Boc-2,8-Diazaspiro[4.5]decane

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Synthesis and physicochemical characterization of meso-functionalized corroles: Precursors of organic-inorganic hybrid materials

Cobalt(III) corroles exhibit an infinite selectivity for the coordination of carbon monoxide towards dioxygen and dinitrogen. This peculiar property thus allows their use as sensing devices for CO detection. Here are described the syntheses and physico-chemical characterization of meso mono-, bis-and tris(triethoxysilyl)-functionalized corroles, precursors of organic-inorganic materials. The corrole ring formation was achieved in every case using the “2+1” method involving the reaction of two equivalents of an encumbered dipyrromethane with one equivalent of an aromatic aldehyde in the presence of a catalytic amount of trifluoroacetic acid. The functionalization of the corrole by triethoxysilyl chains was carried out by a condensation reaction of an isocyanate, bearing a triethoxysilyl termination, either on an amino or hydroxy group. Each final compound and intermediate were characterized by various physico-chemical techniques such as 1H NMR, UV/Vis, MALDI/TOF or EI mass spectrometry and elemental analysis. Wiley-VCH Verlag GmbH & Co. KGaA, 2005.

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High selectivity imaging of nitroreductase using a near-infrared fluorescence probe in hypoxic tumor

A highly selective and sensitive near-infrared (NIR) fluorescence probe (Cy-NO2) for imaging nitroreductase was developed and was successfully applied to investigating the relationship between epithelial-mesenchymal transitions (EMTs) in tumour progression and intracellular hypoxic level.

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Structural investigation on thiazolo[5,4-d]pyrimidines to obtain dual-acting blockers of CD73 and adenosine A2A receptor as potential antitumor agents

Adenosine pathway, including its generating enzyme (CD73) and its receptors represents a key target for cancer immunotherapy. Here we aimed to search for novel compounds able to co-target the CD73 and the A2A adenosine receptor (A2A AR) as dual-blockers of adenosine generation and activity. The design project was to combine in the same molecule the thiazolo[5,4-d]pyrimidine core, an essential pharmacophoric feature to block the A2A AR, with a benzenesulfonamide group which is a characteristic group of CD73 inhibitors. Most of the reported compounds resulted in inverse agonists of the human (h) A2A AR endowed with high affinity, selectivity and potency. However they were weak inhibitors of CD73 enzyme. Nevertheless, this study can be considered as a starting point to develop more active compounds.

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Archives for Chemistry Experiments of 236406-39-6

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EDTA and DTPA modified ligands as sequestering agents for uranyl decorporation

Synthesis of modified EDTA and DTPA ligands and determination of their binding affinities for the uranyl cation are described. Thanks to a screening method, based on a chromophoric complex displacement procedure, chelating properties were studied in aqueous media under various pH conditions for evaluation of their in vivo uranyl-removal efficacy. Each ligand showed a more or less pronounced affinity for uranium. Specific ligands based on EDTA or DTPA analogues containing sulfocatecholamide (CAMS) were found to exhibit a significant affinity towards uranyl ion in acidic, neutral or basic conditions.

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The synthesis of closo- and nido-(aminoalkyl)dicarbaboranes: A re-examination of contradictory literature reports, crystal structure of [7-{H3N(CH2)3}-7,8-C2B9H 11]¡¤NH2NH2

The reaction of Li[1-tBuMe2Si-1,2-C2B10H10 ] with N-(bromoethyl)phthalimide or N-3-(bromopropyl)phthalimide generates unusual carboranyl heterocycles, resulting from nucleophilic substitution followed by insertion of a phthalimide carbonyl into the C-Si bond. The structure of one was determined by single crystal X-ray diffraction. Reaction of the heterocycles with nBu4NF affords closo-1-{C6H4(CO)2N(CH2)n }-1,2-C2B10H11 (1b n = 2 and 1c n = 3) together with the anions nido-[7-{C6H4(CO)2N(CH2)n }-7,8-C2B9H11]- as minor side-products on prolonged reaction. The prolonged reaction of 1b and 1c with hydrazine results in deboronation to give hydrazine solvates of zwitterionic nido-[7-{H3N(CH2)n}-7,8-C2B9 H11]. A single crystal X-ray diffraction study for one reveals an elegant dimeric architecture supported by hydrazine-bridged hydrogen bonds. The reaction of the heterocycles with ethanolic KOH results in cluster deboronation and partial deprotection of the amine group to give nido-[7-(2-O2CC6H4CONH)-(CH2)n -7,8-C2B9H11]2- as potassium salts which can be metathesised to less hygroscopic Me3NH+ salts. The molecular structure of one of the latter displays hydrogen bonding generating a dimeric unit. Complete deprotection of the amine function in these salts by water-HCl gives zwitterionic aminoalkylcarboranes nido-7-{H3N(CH2)n}-7,8-C2B9 H11.

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