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Optically active or racemic compounds represented by the formula STR1 where R2 is OA and R3 is selected from the group consisting of H and OA; where A is H or is selected from the group consisting of hydrocarbyl radicals comprising between 1 and 3 carbon atoms, as well as STR2 with the proviso that when R3 is OA, then R2 and R3 may be bonded together to form the group R4 is selected from the group consisting of alkyl and aromatic residues having from 1 to 20, preferably from 1 to 12, carbon atoms, for example, alkyl, optionally substituted with aromatic residues, and aromatic residues optionally substituted with alkyl radicals; n is an integer from 1 to 4; R5 is an unbranched alkyl chain comprising from 1 and 3 carbon atoms or a cyclopropylmethyl radical; R1 is alkoxy, cycloalkoxy and a cyclic ether of the formula STR3 where m is an integer from 3 to 5; with the proviso that when R1 is alkoxy, then R3 cannot be H; and pharmaceutically-acceptable salts thereof. These compounds are useful for alleviating Parkinsonism, glaucoma, hyperprolactinemia and for inducing weight loss in mammals.

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Disclosed is a compound represented by the general formula (I) or a salt thereof: wherein any one of R1, R2 and R3 represents a group represented by the formula: -(CH2)m-NR11R12 (where in m is 1 or 2; and R11 and R12 independently represent a hydrogen atom or a C1-6 alkyl group or may, together with a nitrogen atom to which R11 and R12 are bound, form a 4- or 5-membered cyclic group); the remaining two or R1, R2 and R3 independently represent a group represented by the formula: -(O)n-R21 (wherein n is 0 or 1; and R21 represents a hydrogen atom, a C1-6 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group, or the like); and R4 represents a C1-6 alkyl group which may have a substituent or the like

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The invention discloses a synthetic method for 3-hydroxylmethal tetrahydrofuran. The synthetic method comprises the following steps: with 2-chloroethanol and diethyl malonate as raw materials, reacting under the action of alkaline in the presence of an organic solvent or in absence of a solvent to obtain an intermediate 2-ethoxy-diethyl succinate; then, reducing the intermediate 2-ethoxy-diethyl succinate by virtue of metal borohydride to obtain 2-hydroxymethyl-1,4-butanediol; and finally, producing 3-hydroxylmethal tetrahydrofuran under the action of a dehydrating agent. According to the synthetic method, the usage amount of the reducing agent metal borohydride is remarkably lowered, and yield of a byproduct sodium metaborate is reduced at the same time. The invention provides the synthetic method for the drug intermediate 3-hydroxylmethal tetrahydrofuran.

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This invention relates to oleic acid derivative comprising a hydrophobic part C17H33 linked to a particular polar head part “A”, especially for use as a medicament, for instance, for the treatment of a disorder caused by the GPR120 receptor and/or the CD36 receptor, comprising administering to a subject in need thereof a therapeutically effective amount of said oleic acid derivative or of said pharmaceutical composition. The invention also relates to the use of said oleic acid derivative as a food composition.

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Tetrahydrofuran | (CH2)3CH2O – PubChem

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The invention relates to compounds of the formula I, wherein R1, R2, R3 and R4 are each independently selected from H, (1-4C)alkyl, (1-4C) alkoxy, trifluoromethyl, trifluoromethoxy, halogen, amino, sulfonamide, cyano, OH and nitro; R5 is H or (1-6C)alkyl; R6 is H, (1-6C)alkyl or (1-6C)alkoxy; R7 is H or (1-6C)alkyl; R8 is (1-6C)alkyl, optionally substituted with (1-6C)alkoxy; R9 is-(CH2)nR10, wherein n is 1, 2 or 3 and R10 is selected from (1-4C)alkoxy, (1-4C) alkylthio, trifluoromethyl, (3-8C)cycloalkyl, phenyl optionally substituted with (1-4C)alkoxy,-NR11R12 and-O(CH2)2 NR11R12, wherein one of R11 and R12 is (1-4C)alkoxy, the other being H or (1-4C)alkyl, or R9 is-CH2(2-7C)heterocycloalkyl, provided that when at least one heteroatom in the heterocycloalkyl moiety is nitrogen, the distance between this nitrogen and the nitrogen in “NHR9″ is at least three carbon atoms, or R9 is-(CH2)3(2-7C) heterocycloalkyl or-(CH2)2CHR13R14, wherein R13 and R14 together with the carbon atom to which they are attached, are (2-7C) heterocycloalkyl; and X is O, S or NH; or a pharmaceutically acceptable salt thereof. The compounds of the invention are Il-8 receptor modulators, in particular inhibitors thereof, and can be used for treating or preventing Il-8 receptor mediated disorders, such as atherosclerosis, inflammation, rheumatoid arthritis and related disorders. ”

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Tetrahydrofuran – Wikipedia,
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A topical insecticide is provided which can be safe to use and avoids many common deleterious side effects of conventional topical insecticides. In one preferred embodiment of the invention, the active ingredient of the insecticide formulation is an amine derivative, having a nitro-methylene group, a nitroamino group or a cyanoamino group, which can be formulated to have low toxicity and excellent insecticidal activity. One particularly suitable insecticide is 1-{(tetrahydro-3-furanyl)methyl}-2-nitro-3-methylguanidine (dinotefuran), an aldulticide that will kill adult fleas dissolved in ethyl lactate.

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Possible structures and modes of formation of C4H7O(1+) ions formed by electron impact induced decomposition of tetrahydrofuran and tetrahydropyran derivates are discussed in view of labelling results and MIKE, CA, and T data.Limitations of these techniques are pointed out.

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An extensive structure-activity relationship study of the 3-position of a series of tricyclic pyrazole-based Chk1 inhibitors is described. As a result, 4?-(1,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-benzonitriles (4) and 4?-(1,4-dihydro-indeno[1,2-c]pyrazol-3-yl)-pyridine-2?-carbonitriles (29) emerged as new lead series. Compared with the original lead compound 2, these new leads fully retain the biological activity in both enzymatic inhibition and cell-based assays. More importantly, the new leads 4 and 29 exhibit favorable physicochemical properties such as lower molecular weight, lower Clog P, and the absence of a hydroxyl group. Furthermore, structure-activity relationship studies were performed at the 6- and 7-positions of 4, which led to the identification of ideal Chk1 inhibitors 49, 50, 51, and 55. These compounds not only potently inhibit Chk1 in an enzymatic assay but also significantly potentiate the cytotoxicity of DNA-damaging agents in cell-based assays while they show little single agent activity. A cell cycle analysis by FACS confirmed that these Chk1 inhibitors efficiently abrogate the G2/M and S checkpoints induced by DNA-damaging agent. The current work paved the way to the identification of several potent Chk1 inhibitors with good pharmacokinetics that are suitable for in vivo study with oral dosing.

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In the presence of 2-phosphino-substituted imidazole ligands and Ru 3(CO)12 or Ru(methylallyl)2(COD) direct hydroformylation and hydrogenation of alkenes to alcohols takes place. In addition to terminal alkenes, also more challenging internal olefins are converted preferentially to industrially important linear alcohols in high yield (up to 88%) and regioselectivity (n:iso up to 99:1).

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Efficient aerobic oxidative methyl esterification of primary alcohols has been achieved with a heterogeneous catalyst consisting of 1 mol % Pd/charcoal (5 wt %) in combination with bismuth(III) nitrate and tellurium metal. The Bi and Te additives significantly increase the reaction rate, selectivity, and overall product yields. This readily accessible catalyst system exhibits a broad substrate scope and is effective with both activated (benzylic) and unactivated (aliphatic) alcohols bearing diverse functional groups.

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Reference:
Tetrahydrofuran – Wikipedia,
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