Abstract: A method for preparing an isobenzofuran-1(3H)-one based compound of the following formula I is provided. R1, R2 and p are defined in the specification.

Abstract: The present invention disclosed herein is a novel commercially feasible, one pot synthesis of library of 3-substituted phthalides of formula I via CuCN mediated oxidative cyclization in high yield.

Abstract: The invention provides a process for the preparation of a compound of Formula 1, comprising coupling a carboxylic acid of Formula 2 with an aniline of Formula 3 in the presence of a coupling agent.

Abstract: This invention provides a novel class of compounds and compositions and synthetic methods related to lactone antioxidant 3-arylbenzofuranones. The compounds may be useful to prevent yellowing and deterioration of organic materials preferably polymers, such as polyurethane foams as one example. The lactone antioxidants may be polymeric, and may also be liquid or paste in physical form at room temperature. Although it is not necessary for its stabilizing properties, the compositions may, in some species, bear one or more reactive primary OH groups on the polymer chains. The chains may also contain oligomeric oxyalkylene ether and aliphatic ester functional groups, in one embodiment of the invention.

Abstract: Disclosed is a method for producing a halogen-substituted phthalide, which includes a reaction step of reacting a halogen-substituted phthalic anhydride with sodium borohydride.

Abstract: The present invention relates to a method comprising (A) reacting a ?-keto ester with a 2-halo ester under basic conditions to obtain a 2-aceto-3-methyl-succinic acid ester; (B) reacting the resulting 2-aceto-3-methyl-succinic acid ester with methyl vinyl ketone under basic conditions, optionally followed by a decarboxylation reaction and hydrolysis, etc., to obtain an ?-methyl-?-keto acid; and (C) reducing the resulting ?-methyl-?-keto acid to obtain wine lactone or a stereoisomer thereof or a mixture thereof.

Abstract: Organic materials which possess outstanding stability to oxidative, thermal or light-induced degradation comprise as stabilizers at least one compound of the formula I wherein the general symbols are as defined in claim 1. The compounds of formula I are especially useful as stabilizers for protecting polymers and lubricants against oxidative, thermal or light-induced degradation and as scavengers for oxidized developer in color photographic material.

Abstract: The present invention relates to a method for manufacturing an ester from a ketone or an aldehyde, which is a reactive substrate, by a Baeyer-Villiger oxidation reaction using hydrogen peroxide, and in this method, as a catalyst, M(BAr4)n, which is a metal borate, is used (M represents an alkali metal or an alkaline earth metal; Ar represents an aryl; and n is the same number as the valence of M). For example, when cyclohexanone was used as the reactive substrate, and Sr[B(3,5-CF3C6H3)4]2 was used as the catalyst, ?-caprolactone was obtained at an isolated yield of 82%.

Abstract: The present invention relates to a method comprising (A) reacting a ?-keto ester with a 2-halo ester under basic conditions to obtain a 2-aceto-3-methyl-succinic acid ester; (B) reacting the resulting 2-aceto-3-methyl-succinic acid ester with methyl vinyl ketone under basic conditions, optionally followed by a decarboxylation reaction and hydrolysis, etc., to obtain an ?-methyl-?-keto acid; and (C) reducing the resulting ?-methyl-?-keto acid to obtain wine lactone or a stereoisomer thereof or a mixture thereof.

Abstract: The invention provides a process for the preparation of a compound of Formula 1, comprising coupling a carboxylic acid of Formula 2 with an aniline of Formula 3 in the presence of a coupling agent.

Abstract: Novel biaryl compounds with phosphodiesterase inhibitory activity of the general formula (I), wherein R1, R2, R3, X, Y, Z1, Z2, Z3, and Z4 have the meanings defined herein, as well as their use as therapeutic agents in the treatment of inflammatory diseases and conditions.

Abstract: The present invention relates to a method comprising (A) reacting a ?-keto ester with a 2-halo ester under basic conditions to obtain a 2-aceto-3-methyl-succinic acid ester; (B) reacting the resulting 2-aceto-3-methyl-succinic acid ester with methyl vinyl ketone under basic conditions, optionally followed by a decarboxylation reaction and hydrolysis, etc., to obtain an ?-methyl-?-keto acid; and (C) reducing the resulting ?-methyl-?-keto acid to obtain wine lactone or a stereoisomer thereof or a mixture thereof.

Abstract: [Object] To improve bitterness or astringency, for example, to reduce stimulative bitterness or astringency of bitter or astringent food and drink, without imparting unnecessary taste or aroma to the food and drink. [Solution] A bitterness- or astringency-improving agent for bitter or astringent food and drink includes phthalides as an active ingredient. Addition of a very small amount of phthalides that are not sensed as aroma to food and drink improves undesirable bitterness or astringency of various bitter or astringent food and drink products and enhances or provides pleasant bitterness or astringency.

Abstract: [Object] To improve saltiness, for example, to reduce feeling of stimulation of saltiness of salty food and drink, without imparting unnecessary taste or aroma to the food and drink. [Solution] A saltiness-improving agent for salty food and drink includes phthalides as an active ingredient. Addition of a very small amount of phthalides that are not sensed as aroma to food and drink improves undesirable saltiness of various salty food and drink products and enhances or provides pleasant saltiness.

Abstract: 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one as crystalline Form A.

Abstract: Disclosed is a method for producing a halogen-substituted phthalide, which includes a reaction step of reacting a halogen-substituted phthalic anhydride with sodium borohydride.

Abstract: Organic materials which possess outstanding stability to oxidative, thermal or light-induced degradation comprise as stabilizers at least one compound of the formula (I) wherein the general symbols are as defined in claim 1. The compounds of formula I are especially useful as stabilizers for protecting polymers and lubricants against oxidative, thermal or light-induced degradation and as scavengers for oxidized developer in color photographic material.

Abstract: The present invention relates to an esterification catalyst composition that includes a zirconium compound and a method for producing an ester compound, which includes the steps of esterifying alcohol and carboxylic acid compounds by using the same, and it may be applied to a mass synthesis process.

Abstract: Described is the use of specific lactone compounds for protecting body-care and household products from photolytic and oxidative degradation. These compounds perform outstanding antioxidant properties.

Abstract: The present invention relates to the use of compounds of the formula (I) wherein the clotted line is an optional bond; R1 is butyl or butyryl if R2 is hydroxyl but is butyl if R2 is hydrogen; or R1 and R2 taken together are 1-butylidene optionally substituted by hydroxyl, methyl, or 3-(?,?-dimethylacrylyloxy)-pentylidenyl; X is a residue selected from the group consisting of X1, X2, X3, X4, and X5; wherein X is X2, X3 or X5 if the dotted line in formula (I) is absent; and X is X1, X4 or X5 if the dotted line signifies a bond in formula (I) above; R3 is hydroxyl or butyryl; and n is 1 or 2, as agents for the prevention, control and treatment of conditions requiring modulation of inflammation in mammals. In another aspect, the present invention relates to the use of compounds of the formula (I) as active ingredients in the manufacture of medicaments/compositions for the prevention, control and treatment of conditions requiring modulation of inflammation.

Abstract: The present invention refers to compounds of the general formula (I) wherein R1 is hydrogen or hydroxy; R2 is butyl or butyryl if R1 is hydroxy, but R2 is butyl if R1 is hydrogen; or R3 and R2 taken together are 1-propylidene or 1-butylidene optionally substituted by hydroxy, methyl, or 3-(?, ?-dimethylacryloyloxy); the dotted line is an optional bond; X is an optionally substituted aliphatic C4-residue selected from the group consisting of X1, X2, X3, X4, and X5; wherein X is X2, X3 or X5 if the dotted line in formula (I) is absent; and X is X1, X4 or X5 if the dotted line signifies a bond in formula (I) above; R3 and R4 are, independently from each other, hydrogen or hydroxy; and R5 is hydroxy or butyryl, for use in the treatment of disorders connected to impaired neurotransmission, as well as to dietary and pharmaceutical compositions containing such compounds, and their uses.

Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.

Abstract: 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one as crystalline Form A.

Abstract: This invention provides a novel class of compounds and compositions and synthetic methods related to lactone antioxidant 3-arylbenzofuranones. The compounds may be useful to prevent yellowing and deterioration of organic materials preferably polymers, such as polyurethane foams as one example. The lactone antioxidants may be polymeric, and may also be liquid or paste in physical form at room temperature. Although it is not necessary for its stabilizing properties, the compositions may, in some species, bear one or more reactive primary OH groups on the polymer chains. The chains may also contain oligomeric oxyalkylene ether and aliphatic ester functional groups, in one embodiment of the invention.

Abstract: A drug effective for the treatment and prevention of psychiatric disorders such as schizophrenia, anxiety and related ailments thereof, depression, bipolar disorder and epilepsy. The drug antagonizes the action of group II metabotropic glutamate receptors and shows high activity in oral administration A 2-amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic ester derivative represented by formula [I] [wherein R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; X represents a hydrogen atom or a fluorine atom; Y represents —OCHR3R4 or the like (wherein R3 and R4 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; and n represents integer 1 or 2)], a pharmaceutically acceptable salt thereof or a hydrate thereof.

Abstract: This invention provides a novel class of compounds and compositions and synthetic methods related to lactone antioxidant 3-arylbenzofuranones. The compounds may be useful to prevent yellowing and deterioration of organic materials preferably polymers, such as polyurethane foams as one example. The lactone antioxidants may be polymeric, and may also be liquid or paste in physical form at room temperature. Although it is not necessary for its stabilizing properties, the compositions may, in some species, bear one or more reactive primary OH groups on the polymer chains. The chains may also contain oligomeric oxyalkylene ether and aliphatic ester functional groups, in one embodiment of the invention.

Abstract: The present invention provides cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs, methods of making cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs and compositions of cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs. The present invention also provides methods of using cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs and compositions of cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs.

Abstract: The present invention relates to the use of a compound as effective agent for the prevention or treatment of diabetes mellitus in a mammal. Said compounds being selected from the group of phthalide derivatives and exhibit excellent blood glucose lowering effects and thus are effective agents in the prevention or treatment of diabetes mellitus in mammals.

Abstract: The present invention relates to a first compound having the formula wherein R is halogen, R1S(O)n or (R1)2NC(X)O; R1 is C1-C8alkyl, C1-C8haloalkyl, aryl-C1-C8-alkyl or aryl; n is 0, 1, 2 or 3; X is O or S; and R3 is C2-C5alkyl or C1-C5haloalkyl, or a salt thereof. The present invention is also directed to a second compound having the formula wherein R is fluorine, bromine, iodine, R1S(O)n or (R1)2NC(X)O; R1 is C1-C8alkyl, C1-C8- haloalkyl, aryl-C1-C8alkyl or aryl; n is 0, 1, 2 or 3; X is O or S; and R2 is hydrogen, C1-C4alkyl or C1-C4haloalkyl, with the proviso that R1 is different from C1-C8 alkyl or aryl if X is S, R is different from iodine if R2 is methyl, and R is different from fluorine, bromine or iodine if R2 is hydrogen.

Abstract: Most carbon-centered free radical antioxidants are generated through hydrogen abstraction. Disclosed herein a new class of antioxidant precursor compounds of the formula A-B, wherein upon exposure of the compounds to an increase in temperature, the compounds undergo at least partial dissociation into free radicals Ao and Bo at least one of which may be functional as an antioxidant. Preferably, each of Ao and Bo is a carbon centered free radical.

Abstract: This invention provides a novel class of compounds and compositions and synthetic methods related to lactone antioxidant 3-arylbenzofuranones. The compounds may be useful to prevent yellowing and deterioration of organic materials preferably polymers, such as polyurethane foams as one example. The lactone antioxidants may be polymeric, and may also be liquid or paste in physical form at room temperature. Although it is not necessary for its stabilizing properties, the compositions may, in some species, bear one or more reactive primary OH groups on the polymer chains. The chains may also contain oligomeric oxyalkylene ether and aliphatic ester functional groups, in one embodiment of the invention.

Abstract: A process for the preparation of citalopram and the pharmaceutically acceptable salts therof is disclosed by reacting 5-cyanophthalide with a 4-fluorophenyl magnesium halide, reducing the 3-hydroxymethyl-4-(4-fluorobenzoyl)benzonitrile with an agent reducing ketones to alcohols, submitting the thus-obtained 3-hydroxymethyl-4-[(4-fluorophenyl)hydroxymethyl)benzonitrile to a cyclization reaction to give 1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofurancarbonitrile without 1,1-bis(4-fluorophenyl)-1,3-dihydro-5-isobenzofurancarbonitrile and treating 1,1-bis(4 fluorophenyl)-1,3-dihydro-5-isobenzofurancarbonitrile with a 3-(dimetylamino)propyl halide in the presence of a base.

Abstract: This invention relates to nonsteroidal progesterone receptor modulators of general formula I, a process for their production, the use of progesterone receptor modulators for the production of pharmaceutical agents as well as pharmaceutical compositions that contain these compounds. The compounds according to the invention are suitable for therapy and prophylaxis of gynecological diseases, such as endometriosis, leiomyomas of the uterus, dysfunctional bleeding and dysmenorrhea, as well as for the therapy and prophylaxis of hormone-dependent tumors and for use for female birth control as well as for hormone replacement therapy.

Abstract: This invention provides a novel class of compounds and compositions and synthetic methods related to lactone antioxidant 3-arylbenzofuranones. The compounds may be useful to prevent yellowing and deterioration of organic materials preferably polymers, such as polyurethane foams as one example. The lactone antioxidants may be polymeric, and may also be liquid or paste in physical form at room temperature. Although it is not necessary for its stabilizing properties, the compositions may, in some species, bear one or more reactive primary OH groups on the polymer chains. The chains may also contain oligomeric oxyalkylene ether and aliphatic ester functional groups, in one embodiment of the invention.

Abstract: The invention provides a new and improved method for the preparation of 5-cyano-phtalid, which is a key intermediate in the preparation of the antidepressant compound citalopram.

Abstract: The present invention relates to the novel isolated 12–30 strain of Pestalotiopsis microspora capable of producing novel antioxidant and antimycotic agents. The present invention also relates to the novel isolated 3,5,7 trisubstituted isobenzofuranone and derivatives thereof, methods of isolating the novel isobenzofuranone from cultures P. microspora 12–30, and to novel uses of the compound as an antioxidant and antimycotic agent. The present invention further relates to a novel 1,5,7 trisubstituted 1,3-dihydroisobenzofuran and derivatives thereof, methods of isolating this novel compound from cultures of Pestalotiopsis microspora 12–30, and to uses thereof.

Abstract: The present invention provides a process for producing an oxide from an alcohol compound, the process comprising the steps of causing silica gel to carry the alcohol compound thereon and an oxidative catalyst thereon, and oxidizing the alcohol compound in the presence of an oxidizing agent, giving an oxide higher in oxidizing degree than the alcohol compound, and also provides a process for producing an oxide from an alcohol compound, the process comprising the steps of causing silica gel to carry the alcohol compound, and subjecting the alcohol compound to an electrolytic oxidation, giving an oxide higher in oxidizing degree than the alcohol compound.

Abstract: In one aspect, the present invention provides a process for producing a sodium salt of an immunosupressant of Formula I

Abstract: A process for catalytically generating organic substances by partial oxidation of an organic feedstock in the presence of molecular oxygen at temperatures in the range from 200 to 500° C. in at least one cooling-tube reactor, wherein 40 to 100 wt-% of the total amount of catalyst is disposed as a coating on the outside of the cooling tubes.

Abstract: The present invention provides cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs, methods of making cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs and compositions of cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs. The present invention also provides methods of using cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs and compositions of cyclic 1-(acyloxy)-alkyl prodrugs of GABA analogs.

Abstract: A method for the preparation of 5-cyanophthalide comprising treatment of a compound of formula IV wherein X is O or S; R1-R2 are each independently selected from hydrogen and C1-6 alkyl, or R1 and R2 together form a C2-5 alkylene chain thereby forming a spiro-ring; R3 is selected from hydrogen and C1-6 alkyl, R4 is selected from hydrogen, C1-6 alkyl, a carboxy group or a precursor group therefore, or R3 and R4 together form a C2-5 alkylene chain thereby forming a spiro-ring; with a dehydration agent or alternatively where X is S, thermally cleavage of the thiazoline ring or treatment with a radical initiator, such as peroxide or with light, to form 5-cyanophthalide, which is an important intermediate used in the preparation of the antidepressant drug citalopram.

Abstract: There is described a process for the preparation of 5-formylphthalide by hydrogenation of a halide of 5-carboxyphthalide, dissolved in a dipolar aprotic solvent, in the presence of a catalyst. Furthermore, the use of 5-formylphthalide in the preparation of citalopram is described.

Abstract: Benzofuran-2-ones, compositions comprising benzofuranones, processes for preparing them, and their use as colorants for high or low molecular mass organic material.

Abstract: A dye thin film containing a dye compound represented by the general formula (I), an optical switch, an optical distributor, an optical modulator and an optical switch array having the dye thin film, as well as a method for producing a dye thin film are provided. The method includes the step of coating the solution of the dye compound on a substrate: where R1 and R2 may be identical or different from each other and each represents, respectively, a linear alkyl group or a branched alkyl group, the dye thin film having high thermal stability, having intense absorption at approximately 1.3 ?m and having ultrafast response characteristic.

Abstract: An inhibitor for 20-hydroxyeicosatetraenoic acid production which comprises as the active ingredient a specific hydroxyformamidine derivative or a pharmacologically acceptable salt thereof. It is useful especially as a remedy for kidney diseases, cerebrovascular diseases, or circulatory diseases. The novel hydroxyformamidine derivative or pharmacologically acceptable salt thereof is also provided.

Abstract: The invention relates to a method for the production of 2-coumarone or substituted 2-coumarones, whereby cyclohexanone or substituted cyclohexanone is reacted with a carboxyl-containing acylating agent a) to give methyl 2-(2-oxo-cyclohexyl)-2-hydroxyacetate or substituted methyl 2-(2-oxo-cyclohexyl)-2-hydroxyacetates, which are either a1) directly converted to 2-coumarone or substituted 2-coumarones by means of catalytic gas-phase dehydrogenation, or a2) dehydrated by means of azeotropic distillation under basic conditions, or by use of a strong acid, or a strongly acidic ion exchanger to a mixture of methyl 2-oxocyclohexylidenacetate and the enol-lactone of the 2-oxocyclohexylidenacetic acid, or a mixture of substituted methyl 2-oxocyclohexylidenacetate and the enol-lactone of the substituted 2-oxocyclohexylidenacetic acid, which is finally converted in turn by catalytic gas-phase dehydrogenation to 2-coumarone, or substituted 2-coumarones, or b) are directly converted under acidic or basic conditions into a

Abstract: A dibenzofuranonylium methylate compound represented by the following formula (I), having maximum absorption wavelength of over 1 &mgr;m, high thermal stability and good solubility in organic solvents, and a production method thereof are provided: where R1 and R2 may be identical or different from each other and each represents a linear alkyl group or a branched alkyl group, respectively.

Abstract: There is described a process for the preparation of 5-formylphthalide by hydrogenation of a halide of 5-carboxyphthalide, dissolved in a dipolar aprotic solvent, in the presence of a catalyst. Furthermore, the use of 5-formylphthalide in the preparation of citalopram is described.

Abstract: The invention describes novel compounds of the formula (I) wherein the general symbols are as defined in claim (1) and R1 is an aromatic radical with electron withdrawing substituents, as stabilizers for protecting organic materials, in particular polymers and lubricants, against oxidative, thermal or light-induced degradation and as scavengers for oxidized developer in color photographic material.

Abstract: The present invention provides a process for producing an oxide from an alcohol compound, the process comprising the steps of causing silica gel to carry the alcohol compound thereon and an oxidative catalyst thereon, and oxidizing the alcohol compound in the presence of an oxidizing agent, giving an oxide higher in oxidizing degree than the alcohol compound, and also provides a process for producing an oxide from an alcohol compound, the process comprising the steps of causing silica gel to carry the alcohol compound, and subjecting the alcohol compound to an electrolytic oxidation, giving an oxide higher in oxidizing degree than the alcohol compound.