Abstract: Provided are novel prodrug salts of selective aquaporin inhibitors, their use as pharmaceuticals, and pharmaceutical compositions comprising them, and novel processes for their synthesis and novel intermediates for use in their synthesis. Also provided is use of a compound for the prophylaxis, treatment, and control of aquaporin-mediated conditions. Aquaporin inhibitors, e.g., inhibitors of AQP4 and/or AQP2, may be of utility in the treatment or control of diseases of water imbalance, for example edema (particularly edema of the brain and spinal cord), hyponatremia, and excess fluid retention, as well as diseases such as epilepsy, retinal ischemia and other diseases of the eye, myocardial ischemia, myocardial ischemia/reperfusion injury, myocardial infarction, myocardial hypoxia, congestive heart failure, sepsis, and neuromyelitis optica, as well as migraines.

Abstract: Process for the preparation of a compound of Formula (I): the process comprising the reaction of a compound of Formula (II) with malononitrile in the presence of a base and a palladium catalyst, wherein X, Y and Z, independently of each other, represent fluoro, chloro or C1-4alkyl; and L is a leaving group; with the proviso that 1 or 2 of X and Y are, independently of each other, fluoro or chloro.

Abstract: Process for the preparation of a compound of Formula (I), the process comprising the reaction of a compound of Formula (II) with malononitrile in the presence of a base and a palladium catalyst, Formula (II) wherein X, Y and Z, independently of each other, represent fluoro, chloro or C1-4alkyl; and L is a leaving group; with the proviso that 1 or 2 of X and Y are, independently of each other, fluoro or chloro.

Abstract: The present invention relates to a process for obtaining a compound of formula (1), (2) or (3) by means of a electrocarboxylation with CO2. The present invention also relates to the new intermediates (1) and (2). The present invention further relates to the use of intermediates (1) and (2) as starting materials for the synthesis of SPAN derivatives.

Abstract: Process for the synthesis of the compound of formula (I): Application in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.

Abstract: There is provided novel fluoro-substituted compounds capable of modulating the G-protein-coupled receptor GPR40, compositions comprising the compounds, and methods for their use for controlling insulin levels in vivo and for the treatment of conditions such as type II diabetes, hypertension, ketoacidosis, obesity, glucose intolerance, and hypercholesterolemia and related disorders associated with abnormally high or low plasma lipoprotein, triglyceride or glucose levels.

Abstract: A method of preparing a tricyanoalkoxy alkane compound is disclosed. The tricyanoalkoxy alkane compound is prepared by reacting an alcohol compound including at least three hydroxyl groups and a nitrile compound in the presence of a potassium alkoxide catalyst. A non-aqueous electrolyte solution comprising the tricyanoalkoxy alkane compound and a lithium secondary battery also are disclosed. The swelling of the battery may be prevented.

Abstract: What is described is a process for preparing organic compounds of the general formula (I) R—R???(I) by converting a corresponding compound of the general formula (II) R—X ??(II) in which X is fluorine, chlorine, bromine or iodine to an organomagnesium compound of the general formula (III) [M+]n[RmMgXkY1]??(III) wherein compounds of the formula (III) are reacted with a compound of the general formula (IV) characterized in that the reaction of (III) with (IV) is performed in the presence of a) catalytic amounts of an iron compound, based on the compound of the general formula (II), and optionally in the presence of b) a nitrogen-, oxygen- and/or phosphorus-containing additive in a catalytic or stoichiometric amount, based on the compound of the general formula (II).

Abstract: The present invention relates to a process for obtaining a compound of formula (1), (2) or (3) by means of a electrocarboxylation with CO2. The present invention also relates to the new intermediates (1) and (2). The present invention further relates to the use of intermediates (1) and (2) as starting materials for the synthesis of SPAN derivatives.

Abstract: A method for producing an unsaturated organic compound represented by the formula (3): (Y1)m-1—R1—R2—(Y2)n-1??(3) wherein Y1 represents R2 or X1, and Y2 represents R1 or B(X2)2, which comprises reacting a compound represented by the formula (1): R1(X1)m??(1) wherein R1 represents an aromatic group or the like, X1 represents a leaving group and m represents 1 or 2, with a compound represented by the formula (2): R2{B(X2)2}n??(2) wherein R2 represents an aromatic group or the like, X2 represents a hydroxyl group or the like, and n represents 1 or 2, in the presence of (a) a nickel compound selected from a nickel carboxylate, nickel nitrate and a nickel halide, (b) a phosphine compound such as 1,4-bis(dicyclohexylphosphino) butane, (c) an amine selected from a primary amine and a diamine such as N,N,N?,N?-tetramethyl-1,2-ethanediamine, and (d) an inorganic base.

Abstract: The present invention is in relation to a dendritic molecule having symmetrically sited branches having four or more generations of dendrimers wherein the branch points are tertiary amines linked together with oxygen atom of ether and the heteroatoms are separated by a substituted or non-substituted linear three methylene linker. In addition the invention also provides a process to prepare such dendritic macromolecules.

Abstract: The present invention relates to titanium catalysts for asymmetric synthesis reactions produced by bringing a reaction mixture obtained by contacting water and a titanium alkoxide into contact with an optically active ligand represented by the general formula (a), wherein R1, R2, R3, and R4 are independently a hydrogen atom, an alkyl group, or the like, and A* represents a group with two or more carbon atoms having an asymmetric carbon atom or axial asymmetry. The invention further relates to a process for asymmetric cyanation of imines, wherein the process comprises reacting an imine with a cyanating agent in the presence of the titanium catalyst.

Abstract: In a process for the preparation of ring compounds via a combinatorial synthesis, the reaction procedure is based on a Suzuki coupling, subsequent halo-demetallation and finally a further Suzuki coupling. The Suzuki couplings are each carried out with a boronic acid or a boronic acid ester. The reaction procedure uses provides novel ring compounds and uses novel synthesis units used for this purpose. The novel ring compounds are suitable for use as constituents in liquid-crystalline mixtures.

Abstract: The present invention provides processes for the preparation of compounds of Formula I, which are useful in the preparation of pharmaceuticals for the treatment of inflammatory diseases. The compounds of Formula I are also useful as pharmaceuticals.

Abstract: In a process for the preparation of ring compounds via a combinatorial synthesis, the reaction procedure is based on a Suzuki coupling, subsequent halo-demetallation and finally a further Suzuki coupling. The Suzuki couplings are each carried out with a boronic acid or a boronic acid ester. The reaction procedure uses provides novel ring compounds and uses novel synthesis units used for this purpose. The novel ring compounds are suitable for use as constituents in liquid-crystalline mixtures.

Abstract: A process for producing a monomer comprising thermally cracking a pre-polymer in the presence of a stabiliser to form a monomer as a distillate , the stabiliser preventing the re-polymerisation of the monomer during cracking while not being carried over in the distillate in normally detectable amounts.

Abstract: Phenylmalonic acid dinitriles are prepared by reaction of, for example, phenyl Kalides with malonic acid dinitrile in the presence of palladium catalysts and bases.

Abstract: Phase-selective soluble polymer supports for catalysts are described. The catalysts utilize polystyrene copolymers having enhanced solubility in nonpolar solvents. Other catalysts of the invention utilize polyisobutylene supports. Methods of catalyzing chemical reactions using latent biphasic solvents are also disclosed.

Abstract: The invention concerns the use of a solid basic catalyst comprising a hydrotalcite structure wherein part at least of the compensating anions are fluoride anions F? for producing Knoevenagel of Michael condensation reactions. The invention also concerns novel solid basic catalysts comprising a hydrotalcite structure characterized by a Mg/Al molar ratio ranging between 2.5 and 3.8 wherein at least part of the compensating anions are fluoride anions F?, and methods for preparing said novel catalysts.

Abstract: The present invention is directed to a process for the synthesis of monoalkylated C—H acidic methylene group-containing compounds, such as malonic esters, and malonic ester nitriles.

Abstract: A process for the production of compounds Ar—R1 by means of a cross-coupling reaction of an organometallic reagent R1-M with an aromatic or heteroaromatic substrate Ar—X catalyzed by one or several iron salts or iron complexes as catalysts or pre-catalysts, present homogeneously or heterogeneously in the reaction mixture. This new invention exhibits substantial advantages over established cross coupling methodology using palladium- or nickel complexes as the catalysts. Most notable aspects are the fact that (i) expensive and/or toxic nobel metal catalysts are replaced by cheap, stable, commercially available and toxicologically benign iron salts or iron complexes as the catalysts or pre-catalysts, (ii) commercially attractive aryl chlorides as well as various aryl sulfonates can be used as starting materials, (iii) the reaction can be performed under “ligand-free” conditons, and (iv) the reaction times are usually very short.

Abstract: A process is described for preparing 3-trifluoromethylphenyl 4-cyanobenzyl ketone by reacting a C1–C2-alkyl 3-trifluoromethylbenzoate with 4-tolunitrile in an aprotic polar solvent or an aprotic polar solvent mixture in the presence of at least an equimolar amount of a base which is selected from potassium alkoxides of primary C1–C4-alkanols.

Abstract: The present invention relates to chiral metal catalysts for stereoselective olefin metathesis reactions, which are recyclable and reusable in such metathesis reactions. The chiral metal-based metathesis catalysts of the invention comprise multidentate optically active or racemic chiral ligands that enable their use in asymmetric synthetic processes, such as for example, in ring-opening and ring-closing metathesis reactions (ROM and RCM, respectively) of alkenes. The catalysts of the invention are organometallic complexes of multivalent metals comprising one or more chiral bidentate ligands that exhibit superior reactivity and stereoselectivity properties. The present invention also provides methods of making such catalysts and methods for utilizing them in catalyzing stereoselective olefin metathesis reactions to provide asymmetric products in relatively high enantiomeric or stereoisomeric excess.

Abstract: A process is described for producing 2-cyano-3-hydroxy-N-(phenyl)but-2-enamide, in which a phenyl-substituted 2-cyano-N-(phenyl)acetamide is reacted in the presence of a base, acetic anhydride and at least one solvent, and the resultant 2-cyano-3-hydroxy-N-(phenyl-derivative)but-2-enamide is crystallized by acidification.

Abstract: Process for the carbonylation of n-pentenoic acid or its derivatives of the formula (I) C4H7—R1??(I) where R1 is —CN or COOR2 where R2 is hydrogen, alkyl or aryl by reaction of a compound of the formula (I) with carbon monoxide and a compound (II) containing a hydroxyl group in the presence of a catalyst system, wherein the catalyst system is obtainable by reaction of a) a source for a metal ion of a metal (III) of the 8th subgroup of the Periodic Table of the Elements with b) a bidentate phosphine ligand of the formula (IV) (R3R4R5C)(R6R7R8C)P-L1-X-L2-P(CR9R10R11) (CR12R13R14)??(IV) where R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14 independently of one another is an organic radical which in each case contains a carbon atom, via which the respective radical is linked to the relevant tertiary carbon atom mentioned in formula (IV); L1, L2 independently of one another are a lower alkylene group; X is an arylene group.

Abstract: The present invention lies in a process for producing a compound represented by the following formula [IV], which comprises the following steps (1) to (3), as well as in an intermediate therefor.

Abstract: Disclosed in a process for making (1) a compound of the formula NC—CH2—CH2—CH2—CH2—CO2R′, wherein R′ is H or C1 to C12 alkyl, or (2) adipic acid or (3) dimethyl adipate, using as the substrate, 3-pentenenitrile, (2) 3-pentenoic acid or methyl 3-pentenoate, respectively, by contacting the substrate with carbon monoxide and a nucleophile in the presence of a Group VIII metal, a selected ligand, and an acid promoter. The nucleophile, which (a) an alcohol or water, or (b) water or (c) methanol, respectively, in the presence of a Group VIII metal, preferably palladium, a selected phosphine ligand, and an acid promoter.

Abstract: The invention pertains to the use of Group 8 transition metal carbene complexes as catalysts for olefin cross-metathesis reactions. In particular, ruthenium and osmium alkylidene complexes substituted with an N-heterocyclic carbene ligand are used to catalyze cross-metathesis reactions to provide a variety of substituted and functionalized olefins, including phosphonate-substituted olefins, directly halogenated olefins, 1,1,2-trisubstituted olefins, and quaternary allylic olefins. The invention further provides a method for creating functional diversity using the aforementioned complexes to catalyze cross-metathesis reactions of a first olefinic reactant, which may or may not be substituted with a functional group, with each of a plurality of different olefinic reactants, which may or may not be substituted with functional groups, to give a plurality of structurally distinct olefinic products.

Abstract: The invention pertains to the use of Group 8 transition metal alkylidene complexes as catalysts for olefin cross-metathesis reactions. In particular, ruthenium and osmium alkylidene complexes substituted with an N-heterocyclic carbene ligand and at least one electron donor ligand in the form of a heterocyclic group are used to catalyze cross-metathesis reactions to provide a olefin products that are directly substituted with an electron-withdrawing group.

Abstract: The present invention relates to processes for the production of &agr;-aryl-&bgr;-ketonitriles, which serve as synthetic intermediates in the preparation of a series of biologically important molecules such as corticotropin releasing factor (CRF) receptor antagonists.

Abstract: The invention relates to a method for the 1,3 dipolar cycloaddition of organic compounds, characterised in that the reaction is carried out in a microreactor.

Abstract: Disclosed is a process for the preparation of a compound of the formula (1) wherein R1 is unsubstituted or substituted alkyl, comprising reacting a compound of the formula (2) with a compound of the formula (3) in the presence of an aqueous base and a phase transfer catalyst.

Abstract: The invention aims to provide a perylene derivative preparation process featuring satisfactory yields and improved preparation efficiency, a perylene derivative obtained by the process, and an organic EL device using the same.

Abstract: The present invention relates to a process for preparing &bgr;-ketonitriles.

Abstract: Disclosed in a process for making (1) a compound of the formula NC—CH2—CH2—CH2—CH2—CO2R′, wherein R′ is H or C1 to C12 alkyl, or (2) adipic acid or (3) dimethyl adipate, using as the substrate, 3-pentenenitrile, (2) 3-pentenoic acid or methyl 3-pentenoate, respectively, by contacting the substrate with carbon monoxide and a nucleophile in the presence of a Group VIII metal, a selected ligand, and an acid promoter. The nucleophile, which (a) an alcohol or water, or (b) water or (c) methanol, respectively, in the presence of a Group VIII metal, preferably palladium, a selected phosphine ligand, and an acid promoter.

Abstract: The invention pertains to the use of Group 8 transition metal carbene complexes as catalysts for olefin cross-metathesis reactions. In particular, ruthenium and osmium alkylidene complexes substituted with an N-heterocyclic carbene ligand are used to catalyze cross-metathesis reactions to provide a variety of substituted and functionalized olefins, including phosphonate-substituted olefins, directly halogenated olefins, 1,1,2-trisubstituted olefins, and quaternary allylic olefins. The invention further provides a method for creating functional diversity using the aforementioned complexes to catalyze cross-metathesis reactions of a first olefinic reactant, which may or may not be substituted with a functional group, with each of a plurality of different olefinic reactants, which may or may not be substituted with functional groups, to give a plurality of structurally distinct olefinic products.

Abstract: Functionalized allylic olefins are condensed by metathesis using the catalyst 1,3-dimesityl-4,5-dihydroimidazol-2-ylidene ruthenium benzylidene [Ru*].

Abstract: Functionalized allylic olefins are condensed by metathesis using the catalyst 1,3-dimesityl-4,5-dihydroimidazol-2-ylidene ruthenium benzylidene [Ru*].

Abstract: This invention provides improved methods for the derivatization and solubilization of fullerenes, which are particularly useful for those fullerenes that are normally insoluble and which are specifically applied, among others, to endohedral fullerenes, including endohedral metallofullerenes; empty fullerenes, including small-bandgap fullerenes and other insoluble fullerenes and to very high molecular weight fullerenic materials generated in fullerenic soot, including giant fullerenes, fullerenic polymers, carbon nanotubes and metal-carbon nanoencapsulates. More specifically the invention relates to improved methods for cyclopropanation of fullerenes. Specific reaction conditions are provided which allow for cyclopropanation reactions to be successfully performed for the first time on insoluble classes of fullerenes.

Abstract: Continuous processes for forming cyanoacrylate from polycyanoacrylate include stripping a solvent from a reaction mass; cracking a polymer in the reaction mass to form a cracked cyanoacrylate monomer and residue substances; and distilling the cracked cyanoacrylate monomer to produce a cyanoacrylate monomer product. These steps can be performed in short-path, wiped-film evaporators. Polycyanoacrylate used in the processes can be formed using cyanoacetate produced by processes for continuously producing cyanoacetate by forming a higher homologue cyanoacetate from a lower homologue cyanoacetate. The cyanoacetate can be formed in short-path, wiped-film evaporators.

Abstract: An improved method is described for making 9-deoxy-PGF1-type compounds. In contrast to the prior art, the method is stereoselective and requires fewer steps than the known methods for making these compounds.

Abstract: A method of preparing a compound of formula I is described.

Abstract: A process for preparing 4-substituted 2-alkylbiphenyls and 2-alkoxybiphenyls of the formula (I), 1

Abstract: Functionalized allylic olefins are condensed by metathesis using the catalyst 1,3-dimesityl-4,5-dihydroimidazol-2-ylidene ruthenium benzylidene [Ru*].

Abstract: A process for preparing fatty amines by the cross-metathesis of normal alpha olefins and acrylonitrile to form an intermediate fatty acid nitrile which is hydrogenated to the corresponding fatty amine.

Abstract: The present invention relates to a process for producing tricarbonitriles corresponding to formula I 1

Abstract: A process for the synthesis of arylpiperidine carbinol intermediates and derivatives is disclosed.

Abstract: Described are &agr;-oxygen-substituted cyclohexane propionitriles having the structure: wherein R20 and R21 are the same or different C1-C3 lower alkoxy; or wherein R20 is hydrogen and R21 is hydroxy, C1-C3 lower alkoxy or C1-C3 lower acyloxy; and wherein R1, R2, R3, R4, R5, R6 and R7 are the same or different hydrogen or C1-C4 lower alkyl, and uses thereof for their organoleptic properties in augmenting or enhancing or imparting aromas in or to perfume compositions, colognes, microporous polymers or perfumed articles including solid or liquid anionic, cationic, nonionic or zwitterionic detergents, fabric softener compositions, fabric softener articles, hair care compositions and the like.

Abstract: A liquid phase process is disclosed for producing halogenated alkane adducts of the formula: CAR1R2CBR3R4 (where A, B, R1, R2, R3, and R4 are as defined in the specification) which involves contacting a corresponding halogenated alkane, AB, with a corresponding olefin, CR1R2═C3R4 in a dinitrile or cyclic carbonate ester solvent which divides the reaction mixture into two liquid phases and in the presence of a catalyst system containing: (i) at least one catalyst selected from monovalent and divalent copper; and optionally (ii) a promoter selected from aromatic or aliphatic heterocyclic compounds which contain at least one carbon-nitrogen double bond in the heterocyclic ring. When hydrochlorofluorocarbons are formed, the chlorine content may be reduced by reacting the hydrochlorofluorocarbons with HF. New compounds disclosed include CF3CF2CCl2CH2CCl3, CF3CCl2CH2CH2Cl and CF3CCl2CH2CHClF. These compounds are useful as intermediates for producing hydrofluorocarbons.

Abstract: A catalyst system, in particular for carrying out cross-coupling reactions is obtainable by reactinga) a palladium(II) compound withb) a water-soluble phosphine ligand andc) a sulfoxide or polyhydric alcohol.