Abstract: A method for obtaining a 5-bromolevulinic acid methyl ester or a 5-chlorolevulinic acid methyl ester from either a bromination mixture or a chlorination mixture, containing either a 5-bromo-levulinic acid methyl ester or a 5-chlorolevulinic acid methyl ester, respectively, produced by either brominating or chlorinating levulinic acid or a levulinic acid methyl ester, and further including the steps of dissolving the bromination or chlorination mixture in an organic solvent or solvent mixture and cooling the solution, preferably to ?20° C.–?40° C., with the 5-bromolevulinic acid methyl ester or 5-chlorolaevulinic acid methyl ester being crystallized out of the solution. The 5-bromolevulinic acid methyl ester or 5-chlorolevulinic acid is then isolated by draining off the solution with the remaining bromination mixture or chlorination mixture, as appropriate.

Abstract: Process for carboxy-alkylation, particularly carboxymethylation, of branched alcohols includes the reaction of isoalcohols with potassium-t-butoxide or sodium-t-butoxide and with salt of halogenated alkanoic acid in the presence of the isoalcohol (starting alcohol) as the solvent. Produced are isoalcohol carboxy-alkylates (preferably, carboxymethylates) in excellent yields and purity.

Abstract: The invention relates to compounds of the formula I in which the radicals are defined as specified, and also to their physiologically tolerated salts. The compounds are suitable, for example, as medicaments for preventing and treating type 2 diabetes.

Abstract: Lactones represented by the formula 2a or 2b: are provided, where each Ph is, independently, an unsubstituted or substituted phenyl group. These lactones are suitable for the synthesis of various ?-hydroxy acids and 1,2-diols.

Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of ?- and ?-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.

Abstract: Aspirin triggered lipid mediators (ATLMs) are disclosed which are useful for the treatment of prevention of inflammation associated with various diseases, including ischemia.

Abstract: A process for preparing solid formulations of sodium 3-hydroxy-3-methylbutyrate of the formula in which, in a first process step, 4,4-dimethyloxetan-2-one is reacted with aqueous sodium hydroxide to form a solution of sodium 3-hydroxy-3-methylbutyrate, and then, if appropriate after concentration, the solution is applied, in a further process step, to synthetic silica, and in which the resultant product is, if appropriate, dried.

Abstract: The invention provides a process for producing glycolide by depolymerization by heating of a glycolic acid oligomer in the presence or absence of a solvent, which process ensures stable depolymerization. The depolymerization reaction is carried out while the content of alkaline metal ions in a glycolic acid oligomer-containing depolymerization reaction system is controlled to 0.001% by mass or lower; a sulfate or an organic acid salt, each in the form of di- or poly-valent cations, or a mixture thereof is allowed to be present as a stabilizer in the depolymerization reaction system; or the content of alkaline metal ions in the depolymerization reaction system is controlled to 0.001% by mass or lower, and a sulfate or an organic acid salt, each in the form of di- or poly-valent cations, or a mixture thereof is allowed to be present as a stabilizer in the depolymerization reaction system.

Abstract: The present invention relates to: a method for producing ?-hydroxycarboxylic acid, which comprises hydrolyzing cyanohydrin in the presence of a hydrocarbon solvent; a method for producing optically active ?-hydroxycarboxylic acid, which comprises: producing optically active cyanohydrin by performing a reaction between a carbonyl compound and hydrogen cyanide, using a solvent comprising at least one organic solvent selected from a group consisting of an alcoholic solvent, an ester solvent, an ethereal solvent and a carboxylic solvent; removing said organic solvent from said reaction solvent; and hydrolyzing the remaining reaction mixture without isolating optically active cyanohydrin; a method for producing optically active ?-hydroxycarboxylic acid, which comprises hydrolyzing optically active cyanohydrin, using at most 10 equivalents of mineral acid relative to said optically active cyanohydrin under the condition that maximum temperature when reacting is 90° C.

Abstract: A quaternary ammonium hydroxycarboxylate is produced by quaternizing a tertiary amine with a hydroxycarboxylic ester represented by the following Formula 1: 1

Abstract: A process for the preparation of chiral &agr;-hydroxycarboxylic acids: in which R1 is optionally halogen substituted C1-C2-alkyl and R2 is optionally halogen substituted C2-C3-alkyl from a compound: in which R′2 is optionally halogen substituted C2-C3-alkylene, m is 0 or 1 and R is optionally substituted alkyl, aryl, heteroaryl or heterocyclyl and X can be oxygen, sulfur, sulfinyl, sulfonyl, imino, C1-C6-alkylimino, xanthate, silyl, or, if m is equal to 0, halogen, which is reacted in the presence of a cyanide group donor to give the corresponding (R)- or (S)-cyanohydrin or its racemate: which then is converted by means of acidic hydrolysis into an acid: or its racemate, and by cleavage of the group: (R)m-X  (V), and optional resolution, whereby the desired chiral &agr;-hydroxycarboxylic acid of the formula (I) is obtained.

Abstract: The invention relates to a process for producing 3,3,3-trifluoro-2-hydroxypropionic acid. This process includes the step of (a) bringing a 1,1-dihalogeno-3,3,3-trifluoroacetone into contact with a basic aqueous solution. The obtained 3,3,3-trifluoro-2-hydroxypropionic acid may be reacted with a C1-C6 lower alcohol under an acidic condition, thereby producing a 3,3,3-trifluoro-2-hydroxypropionate. This propionate may be reacted with a hydride reducing agent (e.g., sodium borohydride), thereby producing 3,3,3-trifluoro-2-hydroxypropanol. These products (i.e., 3,3,3-trifluoro-2-hydroxypropionic acid and its derivatives) are important intermediates for medicines and liquid crystals.

Abstract: Processes for preparing carboxylic acids and derivatives thereof in which an ammonium salt of the carboxylic acid is heated in the presence of an organic reagent to split the salt and form the acid or, where the organic reagent is an esterifying agent, the corresponding ester. Both the acid and the ester may be dehydrated to form unsaturated counterparts.

Abstract: The invention concerns salts of the compound of formula I 1

Abstract: Solid formulations of sodium 3-hydroxy-3-methylbutyrate are produced by the hydrolysis of 4,4-dimethyl-2-oxetanone with aqueous sodium hydroxide to give a solution of sodium 3-hydroxy-3-methylbutyrate and the solution obtained thus is absorbed onto synthetic silicic acid. Said formulations are lightly hygroscopic and easily handled.

Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of &agr;- and &bgr;-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.

Abstract: The invention relates to a process for producing 3,3,3-trifluoro-2-hydroxypropionic acid. This process includes the step of (a) bringing a 1,1-dihalogeno-3,3,3-trifluoroacetone into contact with a basic aqueous solution. The obtained 3,3,3-trifluoro-2-hydroxypropionic acid may be reacted with a C1-C6 lower alcohol under an acidic condition, thereby producing a 3,3,3-trifluoro-2-hydroxypropionate. This propionate may be reacted with a hydride reducing agent (e.g., sodium borohydride), thereby producing 3,3,3-trifluoro-2-hydroxypropanol. These products (i.e., 3,3,3-trifluoro-2-hydroxypropionic acid and its derivatives) are important intermediates for medicines and liquid crystals.

Abstract: The invention relates to a novel process of diastereoselective hydrogenation of 1,3-hydroxyketones of formula (I) 1

Abstract: Aspirin triggered lipid mediators (ATLMs) are disclosed which are useful for the treatment of prevention of inflammation associated with various diseases, including ischemia.

Abstract: A therapeutic formulation comprising a microemulsion of a therapeutic agent in free and/or conjugatively coupled form, wherein the microemulsion comprises a water-in-oil (w/o) microemulsion including a lipophilic phase and a hydrophilic phase, and has a hydrophilic and lipophilic balance (HLB) value between 3 and 7, wherein the therapeutic agent may for example be selected from the group consisting of insulin, calcitonin, ACTH, glucagon, somatostatin, somatotropin, somatomedin, parathyroid hormone, erythropoietin, hypothalamic releasing factors, prolactin, thyroid stimulating hormones, endorphins, enkephalins, vasopressin, non-naturally occurring opioids, superoxide dismutase, interferon, asparaginase, arginase, arginine deaminease, adenosine deaminase, ribonuclease, trypsin, chymotrypsin, papain, Ara-A (Arabinofuranosyladenine), Acylguanosine, Nordeoxyguanosine, Azidothymidine, Didesoxyadenosine, Dideoxycytidine, Dideoxyinosine Floxuridine, 6-Mercaptopurine, Doxorubicin, Daunorubicin, or I-darubicin, Erythro

Abstract: A method of making a cesium salt is described and involves reacting a cesium sulfate containing solution with lime to form 1) a solution containing at least cesium hydroxide and 2) a residue comprising calcium sulfate. The method further involves removing the residue from the solution and converting the cesium hydroxide that is present in the solution to at least one type of cesium salt. The present invention further relates to uses of the cesium salt as well as methods of making cesium hydroxide using lime. Also, methods of making alkali metal salts and alkali metal hydroxides are also described.

Abstract: Process for enantioselectively hydrogenating prochiralen ketones to (S)-alcohols using platinum catalysts in the presence of cinchonines or quinidines as modifiers and in the presence of hydrogen, which is characterized in that the modifiers used are cinchonines unsubstituted in the 3-position, 3-ethylidenyl- or 9-methoxycinchonines or derivatives thereof in which the quinoline ring is replaced by other rings.

Abstract: The present invention relates to:

Abstract: A nitrous acid salt is added at a temperature of 10 to 80° C. to an aqueous solution which contains an optically active 2-aminocarboxylic acid (4) and a protonic acid, the amount of the latter acid being 1 to 3 equivalents to the former, and which has a proton concentration of 0.5 to 2 mol/kg to conduct a reaction to thereby produce an optically active 2-hydroxycarboxylic acid (1). Thionyl chloride and a basic compound are caused to act on the compound (1) to chlorinate it and simultaneously invert the configuration in the 2-position. Thus, an optically active 2-chlorocarboxylic acid chloride (5) is induced. The compound (5) is hydrolyzed to induce an optically active 2-chlorocarboxylic acid (2). The compound (2) is reacted with a thioacetic acid salt to incorporate an acetylthio group thereinto and simultaneously invert the configuration in the 2-position to thereby produce an optically active 2-acetylthiocarboxylic acid (3).

Abstract: The present invention relates to a method for producing 2-hydroxyisobutyric acid where acetone cyanohydrin is converted to 2-hydroxyisobutyric acid using an enzyme catalyst having nitrilase activity, or having a combination of nitrile hydratase and amidase activities. The invention also encompasses production of methacrylic acid wherein the 2-hydroxyisobutyric acid produced with the catalyst described is dehydrated to produce methacrylic acid.

Abstract: The invention relates to a novel process for preparing optically active trimethyllactic acid and/or its esters by catalytic hydrogenation of trimethylpyruvic acid and/or its esters in the presence of noble metal complex catalysts containing phosphorus ligands.

Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of &agr;- and &bgr;-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.

Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of &agr;- and &bgr;-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.

Abstract: Method of increasing the solubility of salts of alpha hydroxy carboxylic acids, preferably used in the field of nutrition and feeding of living matter, and products obtained by the method, the products enhancing and increasing the bio-availability of macro and micro essential elements contained in the products.

Abstract: The invention relates to cycloalkyl derivatives, a process for their preparation and their use.

Abstract: The invention is directed to acylphenylurea derivatives and their physiologically tolerated salts and physiologically functional derivatives. Compounds of the formula I in which the radicals have the stated meanings, and their physiologically tolerated salts and a process for their preparation are described. The compounds are suitable, for example, for treating type II diabetes.

Abstract: Substituted alkylketo compounds of the formula can be converted to the corresponding amino acid by a stereoselective enzymatic process. The resulting amino acid compounds can be employed as starting materials for pharmaceutically active compounds. This invention is directed to the substituted alkylketo compounds and their method of preparation.

Abstract: A quaternary ammonium hydroxycarboxylate is produced by quaternizing a tertiary amine with a hydroxycarboxylic ester represented by the following Formula 1: 1

Abstract: A process for preparing a malonic acid monoester or &bgr;-ketoester from an epoxide includes the steps of reacting an epoxide with carbon monoxide and an alcohol in the presence of a catalytic amount of a cobalt compound and at least one promoter to produce a &bgr;-hydroxyester, separating the &bgr;-hydroxyester from the cobalt compound and the promoter, and oxidizing the &bgr;-hydroxyester to produce a malonic acid monoester or &bgr;-ketoester.

Abstract: The invention is directed to multiply-substituted fullerene derivatives of novel configurations, and methods for their preparation and use. The methods involve the combinatorial synthesis of a library of fullerene derivatives and comprises the steps of forming a mixture of fullerene derivatives by reacting the Cn fullerene with two or more reactive precursor compounds, and removing the unreacted compounds to yield the fullerene derivatives having the desired activity. Methods for the identification and screening of a combinatorial library of fullerenes by 3He-nuclear magnetic resonance and electrospray mass spectrometry to define members with the optimal desired activity are also provided.

Abstract: Heteroatom-interrupted HETE derivatives and methods of their use for treating dry eye are disclosed.

Abstract: In the method of the present invention, a dimethylolcarboxylic acid is produced by reacting a trimethylolalkane and formaldehyde to prepare a cyclic formal having a formal protecting group, followed by the oxidation of the cyclic formal by using nitric acid as an oxidizing agent to prepare a cyclic carboxylic acid which is then subjected to cleavage to remove the formal protecting group. The formal protecting group protects two of the methylol groups against the oxidation to enable the production of the dimethylolcarboxylic acid with a high selectivity.

Abstract: The invention relates to a novel process for preparing optically active trimethyllactic acid and/or its esters by catalytic hydrogenation of trimethylpyruvic acid and/or its esters in the presence of noble metal complex catalysts containing phosphorus ligands.

Abstract: HETE derivatives and methods of their use for treating dry eye are disclosed.

Abstract: A process for the preparation of 3,4-dihydroxybutanoic acid (I) and 3-hydroxy-&ggr;-butyrolactone (V) thereof from a 3-leaving group substituted pentose source is described. In particular, the process relates to the synthesis of (R)-3,4-dihydroxybutanoic acid and (R)-3-hydroxy-&ggr;-butyrolactone from a 3-leaving group substituted L-pentose sugars. The process uses a base and a peroxide to convert the pentose source to the chiral 3,4-dihydroxybutanoic acid compound. The chiral 3,4-dihydroxybutanoic acid can be further converted to 3-hydroxy-&ggr;-butyrolactone by acidification. The chiral compound is useful as a chemical intermediate to the synthesis of various drugs and other products.

Abstract: A process for the preparation of 3,4-dihydroxybutanoic acid (I) and 3-hydroxy-&ggr;-butyrolactone (V) thereof from a 3-leaving group substituted pentose source is described. In particular, the process relates to the synthesis of (R)-3,4-dihydroxybutanoic acid and (R)-3-hydroxy-&ggr;-butyrolactone from a 3-leaving group substituted L-pentose sugars. The process uses a base and a peroxide to convert the pentose source to the chiral 3,4-dihydroxybutanoic acid compound. The chiral 3,4-dihydroxybutanoic acid can be further converted to 3-hydroxy-&ggr;-butyrolactone by acidification. The chiral compound is useful as a chemical intermediate to the synthesis of various drugs and other products.

Abstract: An optically active 1-phenylethylamine is reacted to a phosphine oxide carboxylic acid of a racemic modification shown by the following general formula (2): and a produced diastereomeric salt is separated using the difference in solubility against a solvent, which is subsequently decomposed by acid, so as to free and separate an optically active phosphine oxide carboxylic acid.

Abstract: A method of preparing an ester of a carboxylic acid functionalized with a moiety selected from the group consisting of halides, sulfonates, ethers, hydroxyl, amines, and aldehydes, said method comprising: (a) providing either a carboxylic acid having a vinyl group or an ester thereof; (b) functionalizing the vinyl carbon closest to the carboxyl group with said moiety, wherein said functionalizing comprises cleaving said vinyl group.

Abstract: A process for preparing .alpha.-hydroxy acids by heating ammonium salts of .alpha.-hydroxy acids of general formula (I), removing the formed ammonia and water, adding water to the residue, and heating the obtained mixture, wherein R is hydrogen, C.sub.1 -C.sub.6 alkyl, alkyl(C.sub.1 -C.sub.6)thioalkyl (C.sub.1 -C.sub.6), phenyl or the like. This process is freed from the problem of disposal of by-products such as ammonium bisulfate and makes it possible to prepare a free .alpha.-hydroxy acid from an ammonium salt thereof economically and in a high yield.

Abstract: Mesogens are provided based on substituted unsaturated carboxylic acids such as acrylic and methacrylic acid. Substitution of a variety of hydrophobic tails onto the carboxylic acid or acid derivative via the vinyl carbon proximal to the carbonyl of the carboxylic acid results in mesogens that are capable of forming thermotropic and single-phase lyotropic mesophases over a broad range of compositions. The mesophases can be polymerized to lock in the ordered phases.

Abstract: A process is described for producing acetals comprising reacting an aldehyde or a ketone with an alcohol in the presence of a titanium compound having an acetylacetone as a ligand, or in the presence of a compound selected from the group consisting of stannous chloride dihydrate, cerium chloride hexahydrate and bismuth chloride. The process can be used in the synthesis of unstable acetals or when water exists in the reaction mixture, and therefore the process can be used for a wide variety of applications.

Abstract: A stabilization method of a vinyl compound with hydroxy group of an improved stability is achieved by preventing it from being denatured on storage, transportation, manufacturing process while maintaining its reactivity. A composition containing the vinyl compound with hydroxy group of an improved stability is obtained by the described stabilization method. The stabilization method is characterized by coexisting a vinyl compound with hydroxy group of formula (1), a primary antioxidant, alcohol and/or water, ##STR1## wherein R is a hydrogen atom or an organic residue, X is a --CN group, a --COR.sub.0 group or a --COOR.sub.0 group, and R.sub.0 is a hydrogen atom or an organic residue. In this stabilization method, not less than 50 ppm of alcohol and/or water is added with respect to the vinyl compound with hydroxy group. The stabilization method may be achieved by coexisting the above-defined vinyl compound with hydroxy group, the primary antioxidant and organic acid.

Abstract: The invention is to provide an asymmetric reaction catalyst useful for the production of medical or agricultural chemicals or intermediates thereof. The catalyst comprises an optically active monophosphino carboxylic acid derivative represented by the formula (I): ##STR1## where R.sup.1 represents a C.sub.1-6 alkyl group or phenyl group which may be optionally substituted with a C.sub.1-4 alkyl group or C.sub.1-4 alkoxy group,R.sup.2 represents a C.sub.1-4 alkyl group,R.sup.3 and R.sup.4 each represents independently a hydrogen atom, C.sub.1-4 alkyl group or phenyl group which may be optionally substituted with a C.sub.1-4 alkyl or C.sub.1-4 alkoxy group and a transition metal compound.

Abstract: The present invention relates to a process for preparing a particularly pure glycolic acid by saponification with chloroacetic acid with an excess of alkali metal hydroxide, with the resulting alkali metal chloride being filtered off, and the 20 to 70% strength by weight glycolic acid solution being subsequently subjected to an electrodialysis at 20.degree. to 40.degree. C. and a cell voltage of 0.5 to 2.5 V per cell pair. The process of the invention permits optimum removal of sodium chloride and chloroacetic acid as necessary for preparing a particularly pure glycolic acid. Other organic acids, nitrogen compounds, aldehydes and salts are not produced in this process and thus do not affect the product quality.

Abstract: A vinyl compound having a hydroxy group of the formula (1) ##STR1## wherein R is a hydrogen atom or an organic residue, X is a --CN group, a --COR.sub.0 group or a --COOR.sub.0 group and R.sub.0 is a hydrogen atom or an organic residue, is prepared by reacting a vinyl compound of the formula (2) ##STR2## wherein X is a --CN group, a --COR.sub.0 group or a --COOR.sub.0 group and R.sub.0 is a hydrogen atom or an organic residue, with an aldehyde series compound in the presence of a tertiary amine compound, and water in a sufficient amount for forming an aqueous phase upon the completion of the reaction. In this method, since the aqueous phase is formed upon the completion of the reaction, the organic phase including the vinyl compound having a hydroxy group and the aqueous phase including the tertiary amine compound can be easily separated.