- The reaction of arylacetones with boron tribromide
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Treatment of arylacetones 1 with boron tribromide gives 1,3-dimethyl-2- arylnaphthalenes 3 in fair to good yields by a tandem aldol condensation- intramolecular cyclization. This reaction is limited to the electron-rich arylacetones. In the case of methox
- Dupont, Romain,Cotelle, Philippe
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Read Online
- Toluene dioxygenase-catalyzed cis-dihydroxylation of benzo[b]thiophenes and benzo[b]furans: Synthesis of benzo[b]thiophene 2,3-oxide
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Enzymatic cis-dihydroxylation of benzo[b]thiophene, benzo[b]furan and several methyl substituted derivatives was found to occur in both the carbocyclic and heterocyclic rings. Relative and absolute configurations and enantiopurities of the resulting dihydrodiols were determined. Hydrogenation of the alkene bond in carbocyclic cis-dihydrodiols and ring-opening epimerization/reduction reactions of heterocyclic cis/trans-dihydrodiols were also studied. The relatively stable heterocyclic dihydrodiols of benzo[b]thiophene and benzo[b]furan showed a strong preference for the trans configuration in aqueous solutions. The 2,3-dihydrodiol metabolite of benzo[b]thiophene was utilized as a precursor in the chemoenzymatic synthesis of the unstable arene oxide, benzo[b]thiophene 2,3-oxide.
- Boyd, Derek R.,Sharma, Narain D.,Brannigan, Ian N.,Evans, Timothy A.,Haughey, Simon A.,McMurray, Brian T.,Malone, John F.,McIntyre, Peter B. A.,Stevenson, Paul J.,Allen, Christopher C. R.
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scheme or table
p. 7292 - 7304
(2012/10/07)
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- COMPOUNDS AND METHODS FOR MODULATING FXR
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Compounds of formula. wherein variables are as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and related diseases.
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Page/Page column 27
(2008/06/13)
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- ANTIDIABETIC BICYCLIC COMPOUNDS
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Tricyclic compounds containing a cyclopropyl carboxylic acid or carboxylic acid derivative (e.g. amide) fused to a bicyclic ring, including pharmaceutically acceptable salts and prodrugs thereof, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
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Page/Page column 22-23
(2008/06/13)
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- NOVEL QUINOLINE DERIVATIVES
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The invention relates to compounds represented by Formula (I): and to pharmaceutically acceptable salts or solvates of said compounds, wherein each of A, R3-8, X3, X5, m, and n are defined herein. The invention also relates to pharmaceutical compositions containing the compounds of Formula (I) and to methods of treating hyperproliferative disorders in a mammal by administering compounds of Formula (I).
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Page/Page column 129
(2008/06/13)
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- Facile construction of the benzofuran and chromene ring systems via Pd II-catalyzed oxidative cyclization
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(Chemical Equation Presented) We herein report the development of one-pot procedures for the conversion of allyl aryl ethers to 2-methylbenzofurans (via sequential Claisen rearrangement and oxidative cyclization) and for the conversion of aryl homoallyl e
- So, Won Youn,Jeong, Im Eom
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p. 3355 - 3358
(2007/10/03)
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- Benzofused heterozryl amide derivatives of thienopyridines useful as therapeutic agents, pharmaceutical compositions including the same, and methods for their use
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The invention relates to compounds represented by the formula I and to prodrugs or metabolites thereof, or pharmaceutically acceptable salts or solvates of said compounds, said prodrugs, and said metabolites, wherein Z, Y, R11 and R14, R15, R16, and R17 are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula I and to methods of treating hyperproliferative disorders in a mammal by administering the compounds of formula I.
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- BENZOFUSED HETEROARYL AMIDE DERIVATIVES OF THIENOPYRIDINES USEFUL AS THERAPEUTIC AGENTS, PHARMACEUTICAL COMPOSITIONS INCLUDING THE SAME, AND METHODS FOR THEIR USE
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The invention relates to compounds represented by the formula I and to prodrugs or metabolites thereof, or pharmaceutically acceptable salts or solvates of said compounds, said prodrugs, and said metabolites, wherein Z, Y, R11 and R14, R15, R16, and R17 are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula I and to methods of treating hyperproliferative disorders in a mammal by administering the compounds of formula I.
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Page 121; 122
(2010/02/04)
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- Dyeing composition for keratinous fibers, containing oxidation dye precursors and hydroxybenzofurane used as couplers, and dyeing process using these compositions
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The invention relates to the use, as coupler in a dyeing composition, of a hydroxybenzofuran of formula (I): STR1 in which R1 and R2, which are identical or different, represent a hydrogen atom or a C1 -C6 alkyl radical. When they denote an alkyl radical, R1 and R2 can occupy any position on the benzofuran ring except the positions 2 and 3 at the same time. The OH group may occupy one of the positions 4, 5, 6 or 7, in combination with one or more para type or ortho type oxidation dye precursors or mixtures thereof, for dyeing keratinous fibers and in particular human hair. The dyeing composition according to the invention makes it possible to confer on the keratinous fibers a color which is fast to light, washes, adverse weather conditions and perspiration.
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