Abstract: Cationized hydroxyalkylcelluloses, which are highly compatible with surfactants, are represented by the following formula (I): wherein R1, R2 and R3 represent a hydrogen atom or a group represented by the formula CH2CH2OCH2CH (OH) CH2N+(CH3)Cl−, etc.; and “n” is a number of from 50 to 2,000; which have a mobility distribution (&Dgr;U) determined by electrophoresis ranging from 0.1×105 to 2.0×105 cm2/sec·V.

Abstract: The invention discloses a starch graft poly(meth)acrylate blast media which is effective in paint removal. The media is superior to a physical blend of the components (i.e., starch and acrylic polymers) and to either a starch polymer or an acrylic polymer used singly. The hardness of the media is between 65-90 Shore D.

Abstract: Disclosed are long chained beta glucan isolates containing beta glucan fibers from about 1 to about 6 mm in length, with purity greater than 50%. Also described are the methods to produce these compositions.

Abstract: Methods for the preparation of (2S,3S)-1,5-benzothiazepine derivatives of the formula (II) and isomers thereof, and for the preparation of (2R,3R)-1,5-benzothiazepine derivatives of the formula (III) and isomers thereof, wherein ring A and ring B are independently a substituted or unsubstituted benzene ring, and R2 is a 2-(dimethylamino)ethyl group or a group of the formula: or a pharmaceutically acceptable salt thereof.

Abstract: The synthesis of C11N5 marine sponge alkaloids (±)-hymenin (1), stevensine (2), hymenialdisine (3), and debromohymenialdisine (4) is described. These natural products are the primary family members of the sponge metabolites that contain a fused pyrrolo[2,3-c]azepin-8-one ring system with either a 2-aminoimidazole (AI) or glycocyamidine appendage. The key steps in the synthesis centered around the generation of novel azafulvenium ions and their regioselective heterodimerization with AI in order to create the tricyclic core. A rarely used protodebromination/oxidation strategy was employed to selectively generate the desired a-bromo substitution pattern seen in hymenialdisine (3). In addition, the AI moiety was shown to be a useful precursor to the glycocyamidine unit found in 3 and 4, which suggests that AI derived natural products may be the biogenic forerunners to glycocyamidine metabolites.

Abstract: A staurosporine derivative with anti-cancer activity and anti-bacterial activity is produced by acidifying a solution containing staurosporine to isomerize staurosporine to its desired derivative, whereby the derivative is recovered from the acidified solution.

Abstract: A cyanine dye having the formula wherein R1-R8 are each independently selected from a group consisting of hydrogen, C1-C6 alkyl group, and C0-C4 alkyl group having a hydrophilic substituent thereon. R11 and R12 are chosen to include a free or protected thiol, amine or hydroxyl substituent capable of reacting with a target molecule through a nucleophilic displacement mechanism. The dye is useful in labeling a variety of target molecules. Processes are described for synthesizing suitable heterocyclic and indole derivatives as precursors for the aforementioned cyanine dyes.

Abstract: Provided is a process for preparing carbonylated derivatives of amino- and haloamino-1,3,5-triazines by contacting the 1,3,5-triazine, carbon monoxide and a metal catalyst system containing a metal promoter for promoting carbonylation, at a temperature carbon monoxide pressure and length of time sufficient to carbonylate at least a portion of the amino and/or haloamino groups of the 1,3,5-triazine. The product resulting from contacting these components is an isocyanate functional 1,3,5-triazine; however, the carbamate functional derivative can be readily produced by contacting these components in the further presence of a hydroxy compound, or by post-reacting the isocyanate functional product with such hydroxy compound.

Abstract: Carboxylic acid derivatives where R—R6, X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.

Abstract: Compounds of formula (I) wherein R1 and R2 are as defined in the description and claims and pharmaceutically acceptable salts thereof, are useful for the treating diseases associated with restenosis, glaucoma, cardiac infarct, high blood pressure and end organ damage, for example, cardiac insufficiency and kidney insufficiency.

Abstract: A process for producing a piperidinecarbinol represented by the general formula (2), which comprises reducing the trans isomer of a compound represented by the general formula (1): wherein R1 is a hydrogen atom, a lower alkyl group or an aralkyl group, R2 is a hydrogen atom, a lower alkyl group, an aryl group or an aralkyl group, and X is a hydrogen atom, a halogen atom, an alkyl group, an aryl group, an aralkyl group, an alkoxy group, a dialkylamino group, an alkylthio group, an arylthio group or CmF2m+1— wherein m is an integer of from 1 to 20.

Abstract: At least one of a Rh catalyst, a Pd catalyst or a Ru catalyst is used as a catalyst in preparing the salt of &ggr;-(piperidyl)-butyric acid (2) by hydrogenating the salt of &ggr;-(pyridyl)butyric acid (1) [preferably the salt of &ggr;-(pyridyl)butyric acid (1) obtained in the undermentioned steps (a) and (b) and containing not more than 3% by weight of salt of bis(pyridylethyl)acetic acid (3)] in a solvent in the presence of a catalyst: (a) reacting the vinylpyridine (4) with the diester of malonic acid (5) in the presence of a base to give the 2-(pyridylethyl)malonic acid diester (6), and (b) hydrolyzing and decarboxylating the 2-(pyridylethyl)malonic acid diester (6) obtained in the step (a) in an acidic aqueous solution to give the salt of &ggr;-(pyridyl)butyric acid (1).

Abstract: 2-Sulfonylpyridine derivatives can be industrially produced efficiently by reacting a sulfonyl cyanide derivative with an &agr;, &bgr;-unsaturated carbonyl compound and a 2-{[(2-pyridyl)methyl]thio}-1H-benzimidazole skeleton can be formed in one step in a good yield by reacting this type of the 2-sulfonylpyridine derivative with a 2-methylthio-1H-benzimidazole derivative in the presence of an organolithium compound.

Abstract: Compounds are provided which are crossreactive with peptides such as those which bind G-protein-linked receptors, together with preparative and therapeutic methods therefor. The compounds have the general structure: wherein at least one of R1, R2, R3, R4, or R5 comprises a functional group which is chemically similar to that found in the peptide of interest.

Abstract: The process according to the invention can be illustrated by way of example by the following equation: The monosodium salt of the 3-cyano-2-hydroxy-5-fluoropyrid-6-one (cf. Formula (I)) and/or tautomers thereof are preferably employed in the process according to the invention. The use of a basic catalyst enables significantly lower amounts of chlorinating agent to be employed in the chlorination according to the invention than is necessary, for example, for chlorination of the free dihydroxy compound according to EP-A 333 020. Furthermore, the product 2,6-dichloro-5-fluoronicotinonitrile is obtained in a high purity and high yields after hydrolysis, which is not the case if the conditions according to EP-A 333 020 are applied. Basic catalysts which can be used for the process according to the invention are, for example, organic bases, for example aliphatic and aromatic amines and amides, and also inorganic bases, for example basic compounds of nitrogen and phosphorus and salts thereof.

Abstract: Novel compounds are constructed to include a central aromatic, aliphatic, or heterocyclic ring system. Attached to the central ring system are two linear groups having nitrogenous moieties that are derivatized with chemical functional groups. The ring system can include further nitrogenous moieties, either as ring atoms or on pendant groups attached to the ring, that may also be derivatized with chemical functional groups. The totality of the chemical functional groups imparts certain conformational and other properties to the these compounds. In accordance with certain embodiments of the invention, libraries of such compounds are prepared utilizing permutations and combinations of the chemical functional groups and the nitrogenous moieties to build complexity into the libraries.

Abstract: A method for producing an optically active amino alcohol compound of the formula [3], an enantiomer thereof or a salt thereof, comprising reacting a mesoepoxide compound of the formula [1] with a compound of the formula [2] in the presence of a mixed catalyst comprising a Lewis acid and a proton donor: wherein R1, R2 and R3 are each H, an optionally substituted lower alky, and the like, or R1 and R1 or R2 and R3 may form an optionally substituted ring; and R4 and R5 are each H, an optionally substituted lower alkyl, and the like, or R4 and R5 may form an optionally substituted ring together with the adjacent N, or an imide group or azide group together with the adjacent N, and R6 is H or a silyl group. The present invention enables stereoselective production of a desired intermediate compound, which is an HIV protease inhibitor, extremely efficiently as compared to conventional methods.

Abstract: Compounds of the formula (I) are prepared by reacting a compound of the formula (V) with a compound of the formula (X) and hydrolyzing the product; or converting the compound of the formula (V) into the hydrazide, and cyclizing and hydrolyzing the latter to give the oxadiazole. para-Oxadiazolylphenylboronic acids are valuable precursors for active ingredients.

Abstract: Described is a decolorizable dye represented by the following formula (I): wherein R1 represents an alkyl, aryl or heterocyclic group; R2 and R3 independently each represents a hydrogen atom or has the same meaning as R1 or may be coupled together to form a ring; L1 and L2 independently each represents a methine group or a nitrogen atom; L3 and L4 independently each represents a methine group; Z represents an atomic group necessary for the formation of a 5- or 6-membered hetero ring; m stands for 0 or 1; Y represents an oxygen, sulfur, selenium or tellurium atom; A represents a hydrogen atom or a group eliminative by solution treatment; V stands for a monovalent group; p stands for 0, 1, 2 or 3, X represents a counterion, and n stands for a numeral of 0 or greater necessary for the neutralization of an electron charge in the molecule.

Abstract: The present invention provides a process for producing a substituted alkylamine represented by formula (3): or a salt thereof, which process comprises reacting a 2-aminothiophenol derivative metal salt represented by formula (1): with an amino acid-N-carboxy anhydride represented by formula (2): and then subjecting the reaction product to cyclization under an acidic condition. A substituted alkylamine typified by 1-(2-benzothioazolyl)akylamine, or a salt thereof can be produced from a 2-aminothiophenol derivative industrially at a high handleability and a high yield, and even when the intended substituted alkylamine is an optically active compound, the intended product can be produced without reducing the optical purity of the optically active raw material.

Abstract: The present invention is directed to a process for producing 2-hydroxybenzamide derivatives (2) or (5) according to either one of the following reaction schemes.

Abstract: The present invention relates to a process for manufacturing substituted triazolinones, which are intermediates in the preparation of herbicidally active compounds. In particular, this invention relates to the alkylation of a non-alkylated triazolinone intermediate product, wherein the improvement comprises conducting the alkylation reaction under pH controlled conditions. In a preferred embodiment, the invention relates to the preparation of a 5-alkoxy(or aryloxy)-2,4-dihydro-3H-1,2,4-triazol-3-one, and the alkylation of this non-alkylated triazolinone intermediate product, to produce a 5-alkoxy(or aryloxy)-4-alkyl-2,4-dihydro-3H-1,2,4-triazol-3-one.

Abstract: The present invention concerns novel compounds of formula (I). wherein R1 is C1-10alkyl, C3-7cycloalkyl or C1-6alkyl substituted with C3-7cycloalkyl; R2 is hydrogen or C1-6alkyl; Alk represents C1-3alkanediyl; —A— represents a bivalent radical of formula —CH═CH—N═CH— (a), —N═CH—N═CH— (b), —CH═N—N═CH— (c), —CH═CH—CH═N— (d); in said bivalent radicals a hydrogen atom may be replaced by C1-6alkyl; and Ar is unsubstituted phenyl; phenyl substituted with up to two substituents selected from halo, C1-6alkyl or C1—6alkyloxy; unsubstituted naphthyl; or naphthyl substituted with up to two substituents selected from halo, C1-6alkyl or C1-6alkyloxy; the stereochemically isomeric forms thereof, and the pharmaceutically acceptable acid addition salts thereof.

Abstract: 3-phenylpyrazoles of formula I wherein R1 is cyano, alkyl or haloalkyl; R2 is cyano or is optionally halogenated alkyl, alkoxy, alkylthio, alkylsulfinyl or alkylsulfonyl; R3 is hydrogen, cyano, halogen, alkyl or haloalkyl; R4 is hydrogen or halogen; R5 is cyano, halogen, or is optionally halogenated alkyl or alkoxy; R6, R7 independently of one another are optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, heterocyclyl or phenyl, optionally substituted alkylcarbonyl, alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl or optionally halogenated alkylsulfonyl; X is a chemical bond, —C≡C—, —CH2—CH(R8)— or —CH═C(R8)—, wherein R8 is hydrogen, cyano, nitro, halogen, alkyl or haloalkyl; Y is oxygen or sulfur; their preparation and their use for controlling undesirable vegetation.

Abstract: The invention relates to a process of preparing a chiral compound of the formula: wherein R1 is selected from the group consisting of hydrogen and lower alkyl, and R2 and R2′ are the same, and R2 and R2′ are selected from a group consisting of hydrogen and primary alkyl, or R2 and R2′ taken together form a C3 to C6 cycloalkyl, comprising the steps of chirally reducing a &bgr;-keto ester to afford a &bgr;-hydroxy ester, activating the &bgr;-hydroxy ester by treatment with a sulfonic acid or a derivative thereof to provide an activated compound having sulfonate leaving group, displacing the sulfonate leaving group with an azido moiety, or treating the activated compound with an alkylamine, deprotecting and cyclizing to afford a pyrrolidinone, and reducing the pyrrolidinone to afford a stereoisomerically preferred 3-aminopyrrolidine derivative.

Abstract: There are disclosed compounds of formula (I) and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.

Abstract: 5-Benzoyl-2,3-dihydro-1H-pyrrolizine-1-carboxamides of the formula where R1 is alkyl and R2 is optionally substituted phenyl, and the method for their preparation and their conversion to ketorolac and its pharmaceutically acceptable salts.

Abstract: The invention relates to a process for the preparation of L-ascorbic acid, which comprises lactonizing a melt of alkyl 2-keto-L-gulonate under acidic conditions.

Abstract: A process for the manufacture of the racemic compound of the formula (I), its R-enantiomer (formula R-(I)) and its S-enantiomer (formula S-(I)), and pharmaceutically acceptable salts and/or solvates thereof, as well as new intermediates obtained and used in the process.

Abstract: In a process for preparing polytetrahydrofuran, tetrahydrofuran copolymers, diesters or monoesters of these polymers having a low color number by polymerization of tetrahydrofuran in the presence of at least one telogen and/or comonomer over a heterogeneous catalyst, the polymerization is carried out in the presence of hydrogen.

Abstract: 4-acetoxy-2&agr;-benzoyloxy-5&bgr;, 20-epoxy-1&bgr;, 7&bgr;, 10&bgr;-trihydroxy-9-oxo-11-taxen-13&agr;-y1(2R,3S)-3-t-butoxycarbonylamino-3-phenyl-2-hydroxypropionate trihydrate obtained by a process of centrifugal partition chromatography.

Abstract: Process for preparing taxol, baccatin III and 10-deacetylbaccatin III by oxidation of 9-dihydro-13-acetylbaccatin III.

Abstract: The present invention relates to compounds of formula (I), in which formula X is hydrogen or hydroxy; R1 and R2, which may be the same or different, stand for hydrogen or a C1-C3 alkyl radical; or R1 and R2, taken together with the carbon atom bearing the group X, can form a C3-C6 carbocyclic ring, R3 stands for a C1-C3 alkyl radical, an aryl or an aralkyl radical, or for YR4, in which Y stands for the radicals —CO—S—, —CS—O— or —CS—S—, and R4 stands for a C1-C3 alkyl radical or an aryl or an aralkyl radical; Q is (CH2)n, n being 1-4. R1, R2 and Q independently may optionally be substituted with one or more fluorine atoms. The compounds show strong activity in inducing differentiation and inhibiting undesirable proliferation of certain cells as well as immunomodulating and antiinflammatory effects.

Abstract: The present invention provides germanium-containing compounds which can function as dopants and where the methods for their use are flexible, reliable and environmentally safe. The process includes the ability to make bisamidegermanes under relatively mild conditions, usually standard temperature and pressure, without toxic by-products, giving pure products at satisfactory yields.

Abstract: A method of preparing amorphous copolymers of ethylene and at least one norbornene (NB)-type comonomer is disclosed. These polymers may be random or alternating depending on the choice of catalyst and/or the relative ratio of the monomers used. This method comprises polymerizing said monomers in a diluent or in bulk in the presence of a neutral nickel catalyst which may be represented by the formula wherein Y may be a saturated or unsaturated hydrocarbyl chain, X may be oxygen or sulfur, E may be phosphorus, arsenic, antimony, oxygen or nitrogen, R and R′ independently each is hydrogen or a hydrocarbyl group, L is a ligand containing a heteroatom P, N or O or L and R together with L may form part of a chelating structure in which case L is an ethylenic double bond.

Abstract: A low-bulk density solid aluminoxane has an average particle diameter of 210 to 10,000 &mgr;m and a bulk density of from 0.01 to 1.0 g/cc. Representative solid aluminoxanes may be prepared from polymethylaluminoxane or mixed alkyl group aluminoxanes. The solid aluminoxanes are useful as catalyst carriers. When used to support a metallocene, the combination may be used, for example, as catalyst for olefin polymerization Also disclosed is a prepolymerized catalyst having an average particle diameter of from 500 to 5,000 &mgr;m, useful for olefin polymerization. An olefin is pre-polymerized in the presence of a metallocene catalyst component and a solid low bulk-density aluminoxane and, optionally, an organoaluminum compound.

Abstract: Organo silicon compound having the following general formula (I): R4—Si (OR1) (OR2) (R3)  (I) where R1 and R2 each one independently represent an atom of hydrogen or an alkyl group, R3 represents an hydrogen atom, an hydroxyl group, an amine group, an alkyl group, an alkoxy or a carboxylate group, and at least one of the OR1, OR2 or R3 groups represents an hydroxyl group, R4 represents an alkyl group substituted or not by a functional group such as, notably, an alkyl phosphate group or an alkyl phosphonate group, or any other group for which the R4—Si bond is not hydrolyzable, and the compound: is in solid form, and/or is possibly associated with at least one stabilizer, and/or is possibly associated with at least one dispersant.

Abstract: The present invention relates to chemically stable, polyfunctional, perfluorinated polyorganosiloxanes (POS) comprising on the one hand fluorinated lateral grafts resulting from the hydrosilylation of perfluorinated olefins with SiH units and having alkyl and/or alkyl ester linkages but not ether linkages, and on the other hand other, non-perfluorinated functional units E capable of giving them diverse and varied physical and chemical properties and opening up avenues in numerous applications. Examples of these POS according to the invention are those of the following formula: According to another of its features, the invention relates to a process for the preparation of these polyfunctional perfluorinated POS. Applications: antifoams, agents for lowering surface tension, dirt repellents, antiadhesives, lubricants, oleophobic and/or hydrophobic agents, coatings etc.

Abstract: A method for purifying 3-methacryloxypropyldimethylhalosilanes or 3-methacryloxypropylmethyldihalosilanes which is characterized by the fact that 1-methyl-2-methacryloxyethyldimethylhalosilanes or 1-methyl-2-methacryloxyethylmethyldihalosilanes contained in products or fractions consisting of 3-methacryloxypropyldimethylhalosilanes or 3-methacryloxypropylmethyldihalosilanes produced by a hydrosilation reaction of allyl methacrylate with dimethylhalosilanes or methyldihalosilanes are decomposed by means of a metal halide which shows the properties of a Lewis acid, after which these compounds are subjected to fractional distillation.

Abstract: A fluorine-containing organic silicon compound represented by the following formula 1, which is useful as various industrial base materials required to have performances such as water and oil repellency, anti-fouling properties or release properties and as raw materials therefor.

Abstract: A cyclopentadienyl metal salt is prepared by reacting a cyclopentadiene and a metal hydride in the presence of an amine compound. Furthermore, a derivative of a cyclopentadiene in which a phenyl group is bonded to its cyclopentadienyl moiety through an element of the 14 group of the Periodic Table is prepared using such a reaction.

Abstract: A method and catalyst system for economically producing aromatic carbonates from aromatic hydroxy compounds. In one embodiment, the present invention provides a method of carbonylating aromatic hydroxy compounds by contacting at least one aromatic hydroxy compound with oxygen and carbon monoxide in the presence of a carbonylation catalyst system that includes a catalytic amount of an inorganic co-catalyst containing lead and a catalytic amount of an inorganic co-catalyst containing titanium. In various alternative embodiments, the carbonylation catalyst system can include an effective amount of a palladium source and an effective amount of a halide composition. Further alternative embodiments can include catalytic amounts of various inorganic co-catalyst combinations.

Abstract: The disclosure is a process for preparing mixtures of monoolefinic C5 mononitriles having nonconjugated C═C— and C≡N bonding by catalytic hydrocyanation of a hydrocarbon mixture containing 1,3-butadiene, by first diminishing the proportion of those components in the hydrocarbon mixture which impair the catalytic hydrocyanation and then subjecting the resulting mixture to catalytic hydrocyanation.

Abstract: The naphthyloxyacetic acid derivatives of the formula (I) wherein A is H, -(alkylene)COOR1, -(alkylene)CONR2R3, -(alkylene)OH, -(alkylene)tetrazole, -(alkylene)CN; E is single bond or alkylene; G is —S—, —SO—, —SO2—, —O— or —NR4—; L is alkylene, —(CH2)m—CH═CH—(CH2)n— or —(CH2)x—CH(OH)— (CH2)y—; M is phenyl, phenyl(thio, oxy, amino), diphenylmethyl, diphenylmethyl(thio, oxy, amino), and pharmaceutical composition comprising them as an active ingradient. The compounds of the formula (I) can combine PGE2 receptor and exhibit the activity to antagonize or agonize for PGE2 receptor. Therefore, they are useful as anti-hyperlipemia, for the prevention of abortion, for analgesics, as antidiarrheals, sleep inducer, diuretic, anti-diabetes, abortient, cathartics, antiulcer, anti-gastritis or antihypertensive etc.

Abstract: The present invention relates to silica gel supported bis-cinchona alkaloid compounds of the formula: wherein Q is dihydroquininyl or dihydroquinindinyl; X is a compound having 4 carbon atoms; and R is methoxy, ethoxy or methyl; and methods of preparation and use thereof. The silica gel supported bis-cinchona alkaloid derivatives of this invention are useful re-useable catalysts for preparing vicinal diols by asymmetric dihydroxylation of olefins.

Abstract: The present invention is concerned with a process for the manufacture of chiral succinic acid derivatives of formula (I) wherein R1 is (C1-C6) alkyl or benzyl, and the novel intermediates used therein.

Abstract: A process for preparing an optically active carnitine ester represented by formula (I): wherein R represents a lower alkyl group; and X represents a halogen atom, is disclosed, comprises asymmetrically hydrogenating a &ggr;-trimethylammonium-3-oxobutanoic ester halide represented by formula (II): wherein R and X are as defined above, in the presence of a ruthenium-optically active phosphine complex as a catalyst. An optically active carnitine ester of any desired isomerism can be obtained through simple operation in high yield at high optical purity. The substrate used is easily available.

Abstract: A loaded ion-exchange resin, which resin has been loaded in its shrunken form. Also a process for removing iodide compounds from a liquid carboxylic acid and/or carboxylic acid anhydride obtained from the Group VIII noble metal catalysed, alkyl iodide co-catalysed carbonylation of alcohols and/or their reactive derivatives which process comprises contacting the liquid carboxylic acid and/or carboxylic acid anhydride with a metal loaded ion-exchange resin as described above wherein the metal is one or more of the metals silver, palladium or mercury.

Abstract: Provided is a process for efficiently producing N-glycyltyrosine of high purity represented by the following formula: a salt thereof, or a solvate thereof, which comprises adding dropwise to an aqueous suspension of tyrosine or a salt thereof 2 equivalents or more of a haloacetyl halide and an aqueous solution of an inorganic base simultaneously in the presence or absence of an organic solvent, and subjecting the resulting N-haloacetyltyrosine to a reaction with an ammonium ion. Also provided are N-glycyl-L-tyrosine dehydrate having the crystal structures showing specific diffraction patterns in X-ray powder diffraction and processes for producing the same which are characterized by comprising crystallizing the dihydrate from an ethanol-water mixed solvent or water.

Abstract: The invention relates to a process for the preparation of cyclododecanone oxide consists in photochemically reacting cyclododecane, dissolved in chloroform, a nitrosating agent and hydrogen chloride in a virtually anhydrous medium, that is to say under conditions such that the water content in the reaction medium does not exceed 1000 ppm.