71441-08-2Relevant academic research and scientific papers
A convenient method for the synthesis of aminomethylmonoalkylphosphinate
Ding, Derong,Yan, Guang
, p. 1906 - 1908 (2012/10/29)
Starting from the readily available 4-methylbenzoic acid, an efficient protocol for the preparation of ethyl 4-(aminomethyl) benzyl (methyl) phosphinate (1), a novel aminomethylmonoalkylphosphinate was reported in this communication. The important step involves the selective monochlorination of phosphonic ester by POCl3 and forming the phosphonochloridate, and followed by nucleophilic addition of CH3MgBr to the acid chloride intermediate.
Synthesis of α-arylphosphonates using copper-catalyzed α-arylation and deacylative α-arylation of β-ketophosphonates
Rout, Laxmidhar,Regati, Sridhar,Zhao, Cong-Gui
experimental part, p. 3340 - 3346 (2012/01/17)
Efficient methods for the direct arylation and deacylative arylation of β-ketophosphonates with iodoarenes in presence of a copper(I) or a copper(II) salt as the catalysts have been developed. The corresponding α-arylphosphonates were obtained in high yields. A tentative mechanism for the deacylative arylation reaction was proposed on the basis of the experimental data. Copyright
Direct conversion of benzylic and allylic alcohols to phosphonates
Barney, Rocky J.,Richardson, Rebekah M.,Wiemer, David F.
supporting information; experimental part, p. 2875 - 2879 (2011/05/19)
Benzyl phosphonate esters often serve as reagents in Horner-Wadsworth- Emmons reactions. In most cases, they can be prepared from benzylic alcohols via formation of the corresponding halide followed by an Arbuzov reaction. To identify a more direct synthesis of phosphonate esters, we have developed a one-flask procedure for conversion of benzylic and allylic alcohols to the corresponding phosphonates through treatment with triethyl phosphite and ZnI2.
Rh-catalyzed Negishi alkyl-aryl cross-coupling leading to α- or β-phosphoryl-substituted alkylarenes
Takahashi, Hideki,Inagaki, Shinya,Yoshii, Naoko,Gao, Fuxing,Nishihara, Yasushi,Takagi, Kentaro
supporting information; experimental part, p. 2794 - 2797 (2009/09/08)
The catalytic cross-coupling between ArZnX and ICH2(CH 2)nP(O)(OEt)2 (n = 0-3) has been investigated to determine the utility of the Rh catalyst during the alkyl-aryl cross-coupling and to develop a new syntheti
Synthesis and evaluation of stilbenylbenzoxazole and stilbenylbenzothiazole derivatives for detecting β-amyloid fibrils
Lee, Ji Hoon,Byeon, Seong Rim,Lim, Soo Jeong,Oh, Seung Jun,Moon, Dae Hyuk,Yoo, Kyung Ho,Chung, Bong Young,Kim, Dong Jin
, p. 1534 - 1537 (2008/12/20)
This paper describes a novel series of stilbenylbenzoxazole (SBO) and stilbenylbenzothiazole (SBT) derivatives for β-amyloid specific binding probes. These 24 compounds were synthesized and evaluated by competitive binding assay against β-amyloid 1-42 (Aβ42) aggregates using [125I]TZDM. All the derivatives displayed higher binding affinities with Ki value in the subnanomolar range (0.10-0.74 nM) than Pittsburgh Compound-B (PIB) (0.77 nM). Among these derivatives, SBT-2, 5-fluoroethoxy-2-{4-[2-(4-methylaminophenyl)vinyl]phenyl}benzothiazole, showed lowest Ki value (0.10 nM). In conclusion, the preliminary results suggest that these compounds are implying a possibility as a probe for detection of Aβ fibrils in Alzheimer's disease (AD) patients.
Heterocycles substituted pyridine derivatives and antifungal agent containing thereof
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Page/Page column 138, (2010/11/27)
An object of the present invention is to provide an antifungal agent which has excellent antifungal effects and is superior in terms of its physical properties, safety and metabolic stability. According to the present invention, there is disclosed a compound represented by the following formula (I), or a salt thereof: wherein R1 represents a hydrogen atom, a halogen atom, an amino group, a C1-6 alkyl group, a C1-6 alkoxy group or a C1-6 alkoxy C1-6 alkyl group; R2 represents a hydrogen atom, a C1-6 alkyl group, an amino group or a di C1-6 alkylamino group; one of X and Y is a nitrogen atom while the other is a nitrogen atom or an oxygen atom; ring A represents a 5- or 6-member heteroaryl ring or a benzene ring which may have a halogen atom, or 1 or 2 C1-6 alkyl groups; Z represents a single bond, a methylene group, an ethylene group, an oxygen atom, a sulfur atom, —CH2O—, —OCH2—, —NH—, —CH2NH—, —NHCH2—, —CH2S—, or —SCH2—; R3 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group, a C3-8 cycloalkyl group, a C6-10 aryl group, a 5- or 6-member heteroaryl group, or 5- or 6-member non-aromatic heterocyclic group which may have 1 or 2 substituents; and R4 represents a hydrogen atom or a halogen atom.
Carboxylic acids and the esters thereof, pharmaceutical compositions thereto and processes for the preparation thereof
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Page 33-34, (2008/06/13)
The present invention relates to carboxylic acids and esters of general formula wherein Ar, R, R1, X1, X3, X4, Y and Y1 are defined as in claim 1, the tautomers, the diastereomers, the enantiomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof, as well as the use thereof for the production and purification of antibodies and as labelled compounds in RIA and ELISA assays and as diagnostic or analytical aids in neurotransmitter research.
Luminescent supramolecular assemblies based on hydrogen-bonded complexes of stilbenecarboxylic acids and dithieno[3,2-b:2′,3′-d]thiophene-2-carboxylic acids with a tris(imidazoline) base
Osterod,Peters,Kraft,Sano,Morrison,Feeder,Holmes
, p. 1625 - 1633 (2007/10/03)
The synthesis of a number of stilbenecarboxylic acids, tetrazolylstilbenes and dithieno[3,2-b:2′,3′-d]thiophene-2-carboxylic acids is reported. These organic acids form non-covalent complexes with an imidazoline base, 1,3,5-tris(4,5-dihydroimidazol-2-yl)benzene 13. Two X-ray crystal structures confirm hydrogen bonds between carboxylate ligands and meta-positioned protonated imidazoline groups. The complexes possess a surprisingly flat disk-like shape with various close contacts between adjacent molecules. Most stilbene and dithieno[3,2-b:2′,3′-d]thiophene derivatives show strong blue or blue-green photoluminescence in solution, whereas fluorescence in the solid state is almost completely quenched.
Oxiranyls disubstituted with a phenyl group and a substituted chromanyl or tetrahydroquinolinyl group having retinoid like activity
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, (2008/06/13)
Compounds of the formula STR1 wherein all the symbols in the formula are as defined in the specification, have retinoid-like activity.
Reactivity of the acids of trivalent phosphorus and their derivatives. Part VI. The reaction of the >P-O- anions with benzyl bromides para-substituted in the phenyl ring
Witt, Dariusz,Rachon, Janusz
, p. 169 - 187 (2007/10/03)
The reaction of p-substituted benzyl bromides with the >P-O- ions in THF, alcohols and toluene as the solvents is described. According to the reduction potential of the p-substituted benzyl bromides and the solvent used the formation of the P-C bond, debromination and/or dimerization occur. The principal process is believed to be X-philic substitution, the dimers are formed through a secondary process via SET from the p-substituted benzyl anions into the p-substituted benzyl bromides.
