Abstract: Disclosed is a fluorine-containing aromatic compound represented by the following general formula (1) and its production method. In the formula (1), R1 is a hydroxyl group or amino group, each of R2 to R5 is independently a hydrogen atom, or a C1-4 straight chain or a C3 or C4 branched chain alkyl group, hydrogen atoms of the alkyl group may partially or totally be replaced with fluorine atoms, n is an integer of 0 to 2, and each of m and l is independently 0 or 1. A polymer derived from this fluorine-containing aromatic compound contains —C(CF3)2OH group at a position away from the polymer main chain. Therefore, it is useful for resist use.

Abstract: A pharmaceutical composition including at least one compound of the Formulas (I), (II), or (III), or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, as defined herein. Also disclosed is a method of treatment of diseases which are pathophysiologically related to GPR35, the GPR35-hERG signaling complex, or both, as defined herein.

Abstract: The invention relates to a process for the preparation of a hydroquinone compound of formula (I) wherein R2, R3, R5 and R6 have the meaning according to claim 1, with the steps of formylating a substituted phenol and oxidising the resulting substituted 4-hydroxy-benzaldehyde under acidic conditions to the corresponding hydroquinone of formula (I). Another object of the invention concerns the intermediate 2,3,5-trimethyl-4-hydroxy-benzaldehyde for synthesis of 2,3,5-trimethyl-hydroquinone (TMHQ) and (dl)?-tocopherol.

Abstract: The invention relates to a process for producing a process for producing an 18F-labelled compound, the process comprising treating a compound of formula (I) wherein EDG is an electron-donating group selected from —OH, —OR4, —NHR5 and —NR55R5; R1, R2, X1 and X2 are as defined herein; and R3 is selected from H, X3 and X4, wherein X3 is a monodentate cleavable surrogate group, and X4 is a bidentate cleavable surrogate group which is bonded (a) to said X1 or X2 and (b) to the ring carbon atom para to EDG; with [18F]fluoride in the presence of an oxidant, thereby producing, when R3 in the compound of formula (I) is H, an 18F-labelled compound of formula (II), wherein EDG is as defined above and R1, R2, X1 and X2 are as defined herein; or thereby producing, when R3 in the compound of formula (I) is said monodentate cleavable surrogate group X3, a compound of formula (IIa), wherein EDG? is O, NR5, —NR55R5 or [OR4]+, and wherein R4, R5, R55, R1, R2, X1, X2 and X3 are as defined herein; or thereby producing, whe

Abstract: Stilbene compounds for the prevention and treatment of colon cancer or colon inflammation and methods of using same are provided.

Abstract: A coating liquid including a fluorine-containing organic magnesium compound represented by the following chemical formula (1), a method for manufacturing an optical component having an optical film obtained from the coating liquid, and a photographic optical system are disclosed: Mg(OR11)(OR22) ??Chemical formula (1) where R11 represents an alkyl group that may have a substituent group having 1 or more and 6 or less carbon atoms having at least a fluorine atom, R22 represents an alkyl group that may have a substituent group having 1 or more and 6 or less carbon atoms that may have a fluorine atom, or an aromatic cyclic group that may have a substituent group, and R11 is different from R22.

Abstract: The present invention is directed to methods of providing anticoagulation effects in subjects in need thereof, comprising administering to the subjects at least twice a day compounds of the present invention, stereoisomers, and racemates thereof.

Abstract: A catalyst composition comprising a cation and an anion of the formula Anq?Qpm+, wherein m, n, p, and q are positive integers, wherein m*p=n*q, wherein Qm+ is an organo onium, and Aq? is an anion, provided that at least one Aq? is selected from the formula (I) wherein each R independently is H, halo, alkyl, aryl, aralkyl, or cycloalkyl, and which also may be halogenated, fluorinated, or perfluorinated, wherein two or more of R and R? groups may together form a ring, wherein each R group independently may contain one or more heteroatom(s), wherein R? can be the same as R, with the proviso that R? cannot be halo, and wherein the catalyst composition is essentially free of hydrocarbon containing alcohol.

Abstract: Process for the preparation of hydroxytyrosol, characterized by reacting 4-chloroacetyl-catechol with a metal formate and formic acid in an aqueous solvent optionally containing a lower alkanol and catalytically hydrogenating the 4-hydroxyacetyl-catechol obtained in the presence of a precious metal, preferably on a carrier.

Abstract: A fluorine-containing compound represented by the formula 1, where R1 is a methyl group or trifluoromethyl group, each of R2 and R3 is independently a hydrogen atom or a group containing (a) a hydrocarbon group having a straight-chain, branched or ring form and having a carbon atom number of 1-25 or (b) an aromatic hydrocarbon group, the group optionally containing at least one of a fluorine atom, an oxygen atom and a carbonyl bond, l is an integer of from 0 to 2, each of m and n is independently an integer of 1-5 to satisfy an expression of m+n?6, and when at least one of R1, R2 and R3 is in a plural number, the at least one of R1, R2 and R3 may be identical with or different from each other.

Abstract: Process for the preparation of hydroxytyrosol, characterized by reacting 4-chloroacetyl-catechol with a metal formate and formic acid in an aqueous solvent optionally containing a lower alkanol and catalytically hydrogenating the 4-hydroxyacetyl-catechol obtained in the presence of a precious metal, preferably on a carrier.

Abstract: A method for producing a halogen-substituted benzenedimethanol represented by the formula (2): wherein X1, X2, X3 and X4 are the same or different and each independently represent a hydrogen atom or a halogen atom, provided that X1, X2, X3 and X4 are not hydrogen atoms at the same time, by reacting a halogen-substituted terephthalic acid represented by the formula (1): wherein X1, X2, X3 and X4 are the same meanings as defined above, with a borohydride compound in an organic solvent, followed by contacting the obtained reaction mixture with hydrogen chloride at 40 to 70° C.

Abstract: Trisubstituted phenol compounds and methods of using the compounds, e.g., for anesthetizing a subject, are disclosed.

Abstract: The present invention provides a method of treating glaucoma or ocular hypertension which comprises applying to the eye of a person in need thereof an amount sufficient to treat glaucoma or ocular hypertension of a compound of formula I wherein Y, Q, Z, R, R1 and R2 are as defined in the specification. The present invention further comprises pharmaceutical compositions, e.g. ophthalmic compositions, including said compound of formula I.

Abstract: A reagent for organic synthesis with which a chemical reaction can be conducted in a liquid phase and unnecessary compound(s) can be easily separated at low cost from the liquid phase after completion of the reaction. The reagent for organic synthesis reversibly changes from a liquid-phase state to a solid-phase state with changes in solution composition and/or solution temperature, and is for use in organic synthesis reactions. This reagent for organic syntheses facilitates process development. With the reagent, research on and development of, e.g., medicines through, e.g., compound library synthesis, etc. can be accelerated. It can hence contribute to technical innovations in the biochemical industry and chemical industry.

Abstract: The present invention provides an industrially safe, easily operable process for producing an optically active epoxy alcohol derivative useful as an intermediate for pharmaceuticals from inexpensively available materials, and also provides a novel halohydrin derivative serving as an important intermediate for the epoxy alcohol derivative. Furthermore, the present invention provides a process for producing an intermediate for a triazole antifungal agent by allowing a halohydrin to react with a triazole sulfonamide, the process including a small number of steps.

Abstract: This invention relates, e.g., to methods for inhibiting or stimulating an activity of an adrenomedullin (AM) or gastrin releasing peptide (GRP) peptide hormone, comprising contacting the peptide with a small molecule, non-peptide, modulatory agent of the invention. Complexes of these modulatory agents with other components, such as the peptides or blocking antibodies specific for the peptides, are also described, as are pharmaceutical compositions comprising the modulatory agents, and methods for using the modulatory agents to diagnose or treat patients.

Abstract: Disclosed is a method for producing a dibromofluorobenzene derivative (compound II) comprising a step 1 wherein a compound (I) represented by the general formula (I) below is reacted with a brominating agent in a solvent. (I) (II) (In the formulae, R1 and R2 independently represent a C1-6 alkyl group.

Abstract: A process to synthesize substituted phenols such as those of the general formula RR′R″Ar(OH) wherein R, R′, and R″ are each independently hydrogen or any group which does not interfere in the process for synthesizing the substituted phenol including, but not limited to, halo, alkyl, alkoxy, carboxylic ester, amine, amide; and Ar is any variety of aryl or hetroaryl by means of oxidation of substituted arylboronic esters is described. In particular, a metal-catalyzed C—H activation/borylation reaction is described, which when followed by direct oxidation in a single or separate reaction vessel affords phenols without the need for any intermediate manipulations. More particularly, a process wherein Ir-catalyzed borylation of arenes using pinacolborane (HBPin) followed by oxidation of the intermediate arylboronic ester by OXONE is described.

Abstract: Methods are disclosed for the simple, rapid, and selective colorimetric detection of carbohydrates, including fructose, glucose, sialic acid, and oligosaccharides. There is no need for any prior hydrolysis or other chemical modification or of the analytes. Resorcinarenes, xanthene dyes, and related compounds, formally produced by the reaction of 2 equivalents of resorcinol and a suitable electrophilic condensation partner, are used as chromophores or fluorophores for the detection of sugars and other carbohydrates.

Abstract: A method and a catalyst are described for selective oxidation of aromatic compounds (e.g., benzene and its derivatives) into hydroxylated aromatic compounds (e.g., corresponding phenols). For example, benzene can be converted into phenol with a yield of at least 30-40%, and a selectivity on the basis of benzene of at least 95-97%. The selectivity for this reaction based on N2O is at least 90-95%. Therefore, no substantial N2O decomposition or consumption for complete benzene oxidation to CO+CO2 or other side products occurs. Similar results are obtained with benzene derivatives (e.g., fluorobenzene, difluorobenzene, phenol), although the selectivity is somewhat lower in the case of derivatives (e.g., about 80-85% in the case of fluorosubstituted benzenes). A preferred catalyst for this process is a composition containing a high-silica pentasil-type zeolite (e.g, an HZSM-5 type zeolite) which contains no purposefully introduced additives such as transition or noble metals.

Abstract: A method and a catalyst are described for selective oxidation of aromatic compounds (e.g., benzene and its derivatives) into hydroxylated aromatic compounds (e.g., corresponding phenols). For example, benzene can be converted into phenol with a yield of at least 30-40%, and a selectivity on the basis of benzene of at least 95-97%. The selectivity for this reaction based on N2O is at least 90-95%. Therefore, no substantial N2O decomposition or consumption for complete benzene oxidation to CO+CO2 or other side products occurs. Similar results are obtained with benzene derivatives (e.g., fluorobenzene, difluorobenzene, phenol), although the selectivity is somewhat lower in the case of derivatives (e.g., about 80-85% in the case of fluorosubstituted benzenes). A preferred catalyst for this process is a composition containing a high-silica pentasil-type zeolite (e.g, an HZSM-5 type zeolite) which contains no purposefully introduced additives such as transition or noble metals.

Abstract: A method of imparting a water repellent surface to a hydrophilic substrate which comprises contacting the substrate with a solution or dispersion of a suitable calixarene in a liquid medium.

Abstract: A process for condensing at least one carbonyl compound carrying at least one electron-withdrawing group with an aromatic derivative carrying at least one hydroxyl functional group, wherein the electron-withdrawing group present on the carbonyl compound is selected from fluoroalkyl derivatives, esters, including orthoesters, and nitrites and said condensation is carried out in a basic medium.

Abstract: Facile syntheses for fluorinated resorcinol and aminophenol derivatives are provided that yield isomer-free products in good yield. These novel methods use generally available precursors and standard laboratory reagents and equipment to reproducibly produce these synthetically useful reagents in relatively large quantities. The resulting fluorinated resorcinols and aniinophenols possess utility in the preparation of fluorinated fluorescein and rhodol dyes.

Abstract: Phenolic compounds, e.g., the phenols and phenol ethers, are selectively hydroxylated whereby the amounts of the final product para isomer are enhanced, for example in favor of hydroquinone versus pyrocatechol in the event of the hydroxylation of phenol, by reacting such phenolic compounds with hydrogen peroxide, advantageously in a polar, aprotic, organic solvent reaction medium, in the presence of a catalytically effective amount of a sulfonated polymer and a cocatalytically effective amount of an aromatic ketone compound.

Abstract: The invention relates to a novel process for preparing 4,6-diaminoresorcinol, a precursor to polybenzoxazole, from resorcinol according to the following scheme. ##STR1## Resorcinol (I) is reacted with a di-tert-alkylating reagent to form a 4,6,-di-tert-alkylresorcinol (II), which is then halogenated to form a 2-halo-4,6-di-tert-alkylresorcinol (III). The 2-halo-4,6-di-tert-alkylresorcinol is nitrated in one of two ways to form a 2-halo-4,6-dinitroresorcinol (IV), which is then hydrogenated to from the 4,6-diaminoresorcinol.The invention also relates to a novel chemical composition-2-halo-4,6-di-tert-alkylresorcinol (III )--and a process for preparing same.

Abstract: This invention relates to structurally novel acyclic tocotrienol analogs, which are useful for cholesterol/lipid lowering in cases of hypercholesterolemia and hyperlipidemia, and for atherosclerosis. Also provided are pharmaceutical compositions and a method of use employing those compositions.

Abstract: The invention is a new process for preparing 4,6-diaminoresorcinol, a precursor to polybisbenzoxazoles. The desired product is prepared from resorcinol by incorporating a halo group on the 2-position of resorcinol to form 2-haloresorcinol, then nitrating selectively at the 4- and 6-positions of the 2-haloresorcinol to form 2-halo-4,6-dinitroresorcinol, then hydrogenating the 2-halo-4,6-dinitroresorcinol. The selective incorporation of a halo group on the 2-position of resorcinol is accomplished by sulfonating resorcinol at the 4- and 6-positions.

Abstract: Process for preparing chloranil by the oxidative chlorination of a quinone or of a hydroquinone with a hydrochloric acid/hydrogen peroxide mixture, the introduction of hydrogen peroxide being carried out at a temperature above 60.degree. C.

Abstract: The substituted pentaalkylchromans of the general formula: ##STR1## wherein R denotes a lower alkyl group having 1 to 4 C atoms and Hal denotes chlorine, bromine or iodine, are novel intermediates for the preparation of hypolipidaemic pharmaceuticals. A process for their preparation is described in which a trialkylhydroquinone is reacted with a halogenated butenol to give a substituted tetraalkylhydroquinone, which is finally cyclized to the final product.

Abstract: The substituted pentaalkylchromans of the general formula: ##STR1## wherein R denotes a lower alkyl group having 1 to 4 C atoms and Hal denotes chlorine, bromine or iodine, are novel intermediates for the preparation of hypolipidaemic pharmaceuticals. A process for their preparation is described in which a trialkylhydroquinone is reacted with a halogenated butenol to give a substituted tetraalkylhydroquinone, which is finally cyclized to the final product.

Abstract: A process for the preparation of high-purity tetrachloro-1,4-benzoquinone by the action of hydrogen peroxide and hydrochloric acid on hydroquinone, which comprises causing 3.8 top 4.2 times the molar quantity of 30 to 37% hydrochloric acid and 1.9 to 2.1 times the molar quantity of 50 to 35% hydrogen peroxide, to act at 5 to 50.degree. C. on 1 mole of hydroquinone in at least 12 times the molar quantity of 30 to 37% hydrochloric acid, then heating the resulting suspension, which essentially contains 2,5-dichlorohydroquinone, to 45 to 55.degree. C. and again causing to act on it, at 50 to 95.degree. C., 3.8 to 4.2 times the molar quantity of 30 to 37% hydrochloric acid and 1.9 to 2.1 times the molar quantity of 50 to 35% hydrogen peroxide, in each case based on the hydroquinone used, and finally adding to the suspension, which is now essentially composed of trichloro-1,4-benzoquinone, 1.9 to 2.1 times the molar quantity of hydrochloric acid of the said concentration range, and 0.95 to 1.

Abstract: Phenolic compounds, notably admixtures of 2,4-dichlorophenol and 2,6-dichlorophenol, are selectively chlorinated at the ortho positions thereof, with gaseous chlorine and in a molten medium, in the presence of a selectivity-enhancing effective amount of an organic cation.

Abstract: A process for the production of high-purity tetrachloro-1,4-benzoquinone by the action of chlorine and hydrochloric acid on hydroquinone which comprises causing 1.9 to 2.1 times the molar quantity of gaseous chlorine to act at temperatures from 5.degree. to 15.degree. C. on 1 mol of hydroquinone in 6 to 7 times the molar quantity of 30 to 37% hydrochloric acid, then diluting the resulting suspension, essentially containing 2,5-dichlorohydroquinone, with 2 to 3 parts of water, relative to hydroquinone employed, and initially warming to a temperature from 20.degree. to 30.degree. C., subsequently introducing 1.9 to 2.1 times the molar quantity of chlorine gas in an air atmosphere while raising the temperature to 90.degree.-100.degree. C. with simultaneous dilution with 3.5 to 4.5 parts of water, relative to hydroquinone employed, and finally introducing 1 to 2 times the molar quantity of gaseous chlorine, relative to hydroquinone employed, at temperatures from 100.degree. to 115.degree. C.

Abstract: This invention relates to novel 3-aryl-2-fluoro-1-olefins and their pharmacological use as dopamine beta-hydroxylase DBH inhibitors in the treatment of DBH mediated conditions such as hypertension.

Abstract: Phenol derivatives of the formula ##STR1## wherein A and B have the same or different meanings and each represent one of the groups --C.tbd.C--, cis--CH.dbd.CH-- or trans--CH.dbd.CH--, R.sub.1 is hydrogen, an optionally substituted alkyl or phenyl group or a cycloalkyl group, R.sub.2 is hydrogen, methyl or ethyl, R.sub.3 represents hydrogen, acetyl or propionyl, R.sub.4 has the same meaning as R.sub.3 or represents an alkyl group, R.sub.5 is a carboxylic or a hydroxy group or a functional derivative of such groups or R.sub.5 is a nitrile group and R.sub.6 is hydrogen, an alkyl group or the group OR.sub.4 which specifically inhibit 5-lipoxygenase and are useful in pharmaceutical compositions for prophylaxis and treatment of diseases due to the action of leukotrienes. The compounds are prepared by reacting suitable acetylene compounds or metal derivatives thereof with alkyl or aryl halides or by means of Wittig reactions optionally followed by transforming the member R.sub.

Abstract: Electron-rich aromatic compounds are selectively brominated in good yield in the presence of water using potassium tribromide as the brominating agent. In this way monobromination is favored and dibromination is suppressed as compared to the use of elemental bromine as the brominating agent.

Abstract: The present invention provides a process for preparing a 1,1-disubstituted ethylene derivative of the formula ##STR1## which comprises reacting lead with a carbinol derivative of the formula ##STR2## wherein R.sup.1, R.sup.2, R.sup.3, X, Y, m and n are defined in the specification. The reaction is conducted more advantageously in the presence of a metal having higher ionization tendency than lead.

Abstract: The chlorophenols, e.g., 2,4,6-trichlorophenol, are efficiently prepared by chlorinating an ortho-/para-substituted phenolic compound with gaseous chlorine, whether in molten state or in a solvent reaction medium, in the presence of a catalytically effective amount of a primary, secondary or tertiary amine.

Abstract: A 4-halomethyl-3,5-dihalo-2,6-dialkylphenol is hydrolyzed by contact with water to form a 4-hydroxy-methyl-3,5-dihalo-2,6-dialkylphenol under conditions to minimize formation of the corresponding bis-(4-hydroxy-3,5-dialkyl-2,6-dihalobenzyl) ether.

Abstract: Novel melt-spinnable anisotropic-melt-forming polyesters from certain disubstituted hydroquinones and terephthalic acid have high glass transition temperatures.

Abstract: Phenol derivatives of the formula ##STR1## wherein A and B have the same or different meanings and each represent one of the groups --C.tbd.C--, cis--CH.dbd.CH-- or trans--CH.dbd.CH--, R.sub.1 is hydrogen, an optionally substituted alkyl or phenyl group or a cycloalkyl group, R.sub.2 is hydrogen, methyl or ethyl, R.sub.3 represents hydrogen, acetyl or propionyl, R.sub.4 has the same meaning as R.sub.3 or represents an alkyl group, R.sub.5 is a carboxylic or a hydroxy group or a functional derivative of such groups or R.sub.5 is a nitrile group and R.sub.6 is hydrogen, an alkyl group or the group OR.sub.4 which specifically inhibit 5-lipoxygenase and are useful in pharmaceutical compositions for prophylaxis and treatment of diseases due to the action of leukotrienes. The compounds are prepared by reacting suitable acetylene compounds or metal derivatives thereof with alkyl or aryl halides or by means of Wittig reactions optionally followed by transforming the member R.sub.

Abstract: Resorcinol and substituted resorcinols are converted in one single step reaction into 1,2,3- and 1,2,4-trihydroxybenzenes and substituted hydroxy resorcinol compounds with a benzene solution of peroxypropionic acid.

Abstract: A process for the perfluoroalkylation of aromatic derivatives. In a first stage, an aromatic derivative, sulfur dioxide and a metal selected from the group consisting of zinc, aluminum, manganese, cadmium, magnesium, tin, iron, nickel and cobalt, are brought into contact in a solvent, preferably a polar aprotic solvent. In a second stage, a perfluoroalkyl bromide or iodide is added to react with the aromatic derivative.

Abstract: A method for the preparation of 2-halogenoresorcinols having the following formula I ##STR1## where X represents a halogen atom and R and R.sub.1 may be the same or different and represent a hydrogen atom or a free organic functional or functionally modified group or a hydrocarbon group, which may be substituted by one or more free organic functional or functionally modified groups and R and R.sub.1 jointly may also represent a free organic functional or functionally modified group or a hydrocarbon group which may be substituted by one or more free organic functional or functionally modified groups, and esters, ethers, or salts thereof.The method comprises sulfonating the corresponding resorcinols which do not contain a halogen in the 2-position and then halogenating the sulfonic acids thus obtained. The halogenated sulfonic acids thereby obtained are subsequently protodesulfonated by acid hydrolysis and, if desired, any functional groups which may be present can be modified.

Abstract: Ring opened halogenated Resorcyclic Acid Lactone (RAL) derivatives having the structure: ##STR1## are used to increase rumen fermentation efficiency.

Abstract: Hydroquinone is selectively nascently chlorinated to monochlorohydroquinone, by reacting same with an aqueous solution of hydrochloric acid and hydrogen peroxide, in the presence of an organic solvent for, and inert to, said hydroquinone.

Abstract: 4-Acylresorcinol ethers of the formula ##STR1## in which R.sub.1 is lower alkyl, R.sub.2 is fluorinated lower alkyl, R.sub.3 is hydrogen, lower alkoxy, trifluoromethyl or halogen, alk is an alkylene or hydroxyalkylene radical which is uninterrupted or interrupted by oxygen, one of the radicals R.sub.4, R.sub.5 and R.sub.7 is a group of the formula --NH--C(.dbd.O)--R.sub.8, a radical R.sub.4 or R.sub.5 which differs from this is a radical R.sub.9 and a radical R.sub.7 which differs from this is a radical R.sub.10, R.sub.6 is hydrogen, lower alkyl, trifluoromethyl, halogen, carboxyl which is free, esterified or amidated, cyano or lower alkanoyl, R.sub.8 is carboxyl which is free, esterified or amidated or 5-tetrazolyl, R.sub.9 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl and R.sub.10 is hydrogen, lower alkyl, lower alkoxy, halogen, trifluoromethyl, cyano or carboxyl which is free, esterified or amidated, and their salts have antiallergic and antiinflammatory properties.

Abstract: A catechol derivative represented by the formula ##STR1## The compounds of this invention are useful for the prophylaxis and treatment for various allergic diseases, ischemic heart diseases and inflammations caused by slow reacting substance of anaphylaxis (SRS-A), since the compounds inhibit very potently the formation and release of SRS-A.