- A benzofuran -3 - carboxylic acid (by machine translation)
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The invention relates to a benzofuran - 3 - carboxylic acid preparation method, the method using the intermediate 1 as raw materials, under alkaline conditions in the open-loop, the closed-loop process for preparing benzofuran - 3 - carboxylic acid. The method is characterized in that the mild reaction conditions, the operation is simple, high yield, is suitable for industrial production. (by machine translation)
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Paragraph 0009; 0015; 0016; 0018; 0020; 0022; 0024
(2018/07/30)
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- 2-Oxo-Driven Coupling Reactions of 2-Oxo Aldehydes/2-Oxo Iminium Ions and Hydroperoxides at Room Temperature
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An efficient 2-oxo-group-promoted direct coupling reaction between 2-oxo aldehydes and hydroperoxides has been developed. The method has been used successfully for the generation of different 2-oxo esters and acids. This reaction harnesses the hydrogen-bonding-induced self-decomposition tendency of hydroperoxides; the intermediates produced by this process then attack the aldehyde or iminium ion to generate cross-coupled products either by direct coupling or by an amine-catalysed pathway. No external oxidants or metal catalysts are required for our method, and the reaction takes place at room temperature.
- Khan, Shahnawaz,Ahmed, Qazi Naveed
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p. 5377 - 5385
(2016/11/22)
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- ANTI-HIV COMPOUNDS
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Thiazole derivatives represented by Formula (I) are disclosed, where R1, R2, R3, A, X, Y, Z, R6 and R7 are disclosed herein. These thiazole derivatives and pharmaceutical compositions comprising these derivatives are useful in the treatment of HIV mediated diseases and conditions.
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Page/Page column 40; 50
(2009/08/14)
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- Silver-catalyzed protodecarboxylation of heteroaromatic carboxylic acids
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[Chemical Equation Presented] A simple and highly efficient protodecarboxylation procedure for a variety of heteroaromatic carboxylic acids catalyzed by Ag2CO3 and AcOH in DMSO is described. This methodology can also perform the selective monoprotodecarboxylation of several aromatic dicarboxylic acids.
- Lu, Pengfel,Sanchez, Carolina,Cornella, Josep,Larrosa, Igor
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supporting information; experimental part
p. 5710 - 5713
(2010/02/28)
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- NOVEL INDOL CARBOXYLIC ACID BISPYRIDYL CARBOXAMIDE DERIVATIVES, PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PREPARATION METHOD AND COMPOSITION CONTAINING THE SAME AS AN ACTIVE INGREDIENT
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Disclosed herein are a new indole carboxylic acid bispyridyl carboxamide derivative, a preparation method thereof, and a composition for prevention or treatment of obesity, urinary disorders, and CNS disorders, containing the same as an active ingredient. Because the indole carboxylic acid bispyridyl carboxamide derivatives according to the present invention have high affinity for 5-HT2c receptors, act selectively on the 5-HT2c receptors, the derivatives rarely have adverse effects caused by other receptors. Because the derivatives effectively inhibit serotonin activity, they may be useful for treatment or prevention of obesity; urinary disorders such as urinary incontinence, premature ejaculation, erectile dysfunction, and prostatic hyperplasia; CNS disorders such as depression, anxiety, concern, panic disorder, epilepsy, obsessive-compulsive disorder, migraine, sleep disorder, withdrawal from drug abuse, Alzheimer's disease, and schizophrenia, associated with 5-HT2c receptors.
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Page/Page column 8
(2009/10/21)
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- Novel indol carboxylic acid bispyridyl carboxamide derivatives as 5-HT2c receptor antagonists
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Disclosed herein are a new indole carboxylic acid bispyridyl carboxamide derivative, a preparation method thereof, and a composition for prevention or treatment of obesity, urinary disorders, and CNS disorders, containing the same as an active ingredient. Because the indole carboxylic acid bispyridyl carboxamide derivatives according to the present invention have high affinity for 5-HT2c receptors, act selectively on the 5-HT2c receptors, the derivatives rarely have adverse effects caused by other receptors. Because the derivatives effectively inhibit serotonin activity, they may be useful for treatment or prevention of obesity; urinary disorders such as urinary incontinence, premature ejaculation, erectile dysfunction, and prostatic hyperplasia; CNS disorders such as depression, anxiety, concern, panic disorder, epilepsy, obsessive-compulsive disorder, migraine, sleep disorder, withdrawal from drug abuse, Alzheimer's disease, and schizophrenia, associated with 5-HT2c receptors.
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Page/Page column 12
(2009/10/21)
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- Synthesis and structure-activity relationship of 1H-indole-3-carboxylic acid pyridine-3-ylamides: A novel series of 5-HT2C receptor antagonists
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A novel series of 1H-indole-3-carboxylic acid pyridine-3-ylamides were synthesized and identified to show high affinity and selectivity for 5-HT2C receptor. Among them, 1H-indole-3-carboxylic acid[6-(2-chloro-pyridin-3-yloxy)-pyridin-3-yl]-amide (15k) exhibits the highest affinity (IC50 = 0.5 nM) with an excellent selectivity (>2000 times) over other serotonin (5-HT1A, 5-HT2A, and 5-HT6) and dopamine (D2-D4) receptors.
- Park, Chul Min,Kim, So Young,Park, Woo Kyu,Park, No Sang,Seong, Churl Min
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supporting information; experimental part
p. 3844 - 3847
(2009/04/16)
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- PHENYL DIAZEPANE CARBOXAMIDES AND ANNELATED PHENYL PIPERAZINE CARBOXAMIDES CONTAINING OXYGEN AND USED AS DOPAMINE D3 ANTAGONISTS
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The invention relates to annelated phenyl piperazine and phenyl diazepane carboxamides of general formula (I) containing oxygen.The compounds are suitable for medical purposes.
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Page/Page column 33
(2008/06/13)
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- AZABICYCLO-OCTANE INHIBITORS OF IAP
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The invention provides novel inhibitors of IAP that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula (I) in which X1 and X2 are independently O or S; L is a bond or -C(X3
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Page/Page column 42
(2008/06/13)
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- Preparation of 2,3-Dimethylene-2,3-dihydrobenzofuran by the Flash Vacuum Pyrolysis of (2-Methyl-3-benzofuryl)methyl Benzoate
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Pyrolysis of (2-methyl-3-benzofuryl)methyl benzoate (7) gives a 30percent yield of two dimers of 2,3-dimethylene-2,3-dihydrobenzofuran (4), a dimer 12 and a dimer (13), in a ratio of 4.1 to 1.It is shown, by low-temperature 1H-NMR spectroscopy, that the primary pyrolysis product from 7 is 4, which forms 12 and 13 upon warming.The structure of the dimer 12 is confirmed by a deuterium-labeling experiment.Compound 4 can be trapped with methyl acrylate to form a 3.0 to 1 ratio of two Diels-Alder adducts.
- Chou, Chin-Hsing,Trahanovsky, Walter S.
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p. 4208 - 4212
(2007/10/02)
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- CONFORMATIONAL ANALYSIS OF ORGANIC CARBONYL COMPOUNDS. PART 4. A (1)H AND (13)C NUCLEAR MAGNETIC RESONANCE STUDY OF FORMYL AND ACETYL DERIVATIVES OF BENZOFURAN
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A conformational study of formyl and acetyl derivatives of benzofuran provides evidence that in the case of 2- and 7-derivatives the E,Z-conformational mixture is solvent dependent, the Z-form prevailing in solvents with higher polarity.The presence of the same substituents in the 3- and 4-position gives compounds with predominantly Z-conformation and no change is caused by solvents.These results show an interestingly different behaviour by carbonyl derivatives of benzofuran with respect to the same benzothiophene derivatives.The conformational analysis was carried out by the n.m.r. method by employing (1)H and (13)C chemical shifts, long-range proton-proton coupling constants, and lanthanide-induced shifts (LIS) simulation.For the derivatives substituted in position 7, the LIS method is not a suitable approach for the determination of the conformer populations since, in solution, a chelate is formed where bonding of Eu to the oxygen atoms of the carbonyl and of the heterocyclic ring stabilizes the Z-form.A quantitative approach for determining the relative conformer populations of benzofuran-7-carbaldehyde was set up by statistical manipulation of long-range proton-proton coupling constants, proton chemical shifts, and the classical of dielectrics.
- Benassi, Rois,Folli, Ugo,Iarossi, Dario,Schenetti, Luisa,Taddei, Ferdinando
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p. 1479 - 1486
(2007/10/02)
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- Furano Compounds: Part IL - Solvolytic Rearrangement of Ketoximes in Benzofuran Series and PMR Study of Benzofuryl-2-alkyl(aryl) Ketoximes
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Solvolytic rearrangement of tosylates of 3-alkyl(aryl)-benzofuryl-2-alkyl ketoximes and 2-substituted(and unsubstituted)benzofuryl-3-methyl ketoximes with aqueous methanol depends upon their configurations.The tosylates of 2-ethyl(benzyl)benzofuryl-3-methyl ketoximes obtained in alkaline medium do not undergo solvolytic rearrangement under similar conditions.The isomerisation of anti-isomers of the above mentioned ketoximes to syn-forms with hydrogen chloride is unsuccesful.The configurations of syn- and anti-isomers of benzofuryl-2-alkyl(aryl) ketoximes have been studied by PMR spectroscopy.
- Chatterjea, J. N.,Singh, K. R. R. P.
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p. 1053 - 1056
(2007/10/02)
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