Abstract: The present invention relates to a process for the preparation of ospemifene and pharmaceutically acceptable salts thereof which comprises the step of recycling the undesired E-4-(4-hydroxy-1,2-diphenylbut-1-enyl)phenol to generate an isomeric mixture of Z,E-4-(4-hydroxy-1,2-diphenylbut-1-enyl)phenol.

Abstract: Provided is a resin composition having excellent heat resistance by virtue of improved compatibility of a fullerene with a resin. Specifically, provided is a long-chain alkyl-etherified fullerene derivative, including: a fullerene skeleton formed of a spherical shell-shaped carbon molecule; and a long-chain alkyl group having 4 or more carbon atoms, which is bonded to the fullerene skeleton through an ether bond.

Abstract: Disclosed are a process and catalysts useful for carrying out asymmetric methlyallylations. The catalysts used in the invention have the formula (IV): wherein X1, X2, R3 and R4 are as defined herein. Compounds made by the process of the invention can be used to prepare pharmaceutically active compounds such as 11-?-hydroxysteroid hydrogenase type 1 (11-?-HSD1) inhibitors including 1,3-disubstituted oxazinan-2-ones.

Abstract: Provided are a novel fullerene derivative which can adsorb quickly and efficiently an allergen which may cause a pollen allergy without releasing the allergen again, does not contain a metal or the like which may cause a harmful effect to a human body, and is easily applicable, impregnable, or chemically bondable onto surface of various materials; and a process for producing the same. The fullerene derivative is characterized in that a halogen group and many hydroxyl groups are bonded directly to a fullerene nucleus. In the case that the halogen group is chlorine, the fullerene derivative can be synthesized by a partial hydroxylation of a chlorinated fullerene or a partial chlorination of a hydroxylated fullerene.

Abstract: A synergistic microbicidal composition containing a phenolic compound selected from the class consisting of chlorinated phenols, monosubstituted phenols, fused bicyclic phenols, isopropyl methyl catechols, and monosubstituted catechols and an antimicrobial alcohol selected from the class of menthadiene alcohols and other antimicrobial alcohols.

Abstract: Provided is a ruthenium complex that is represented by general formula (1*) and is useful as an asymmetric reduction catalyst. (In the formula, * is an asymmetric carbon atom; R1 is an arenesulfonyl group, and the like; R2 and R3 are a phenyl group, and the like; R10 through R14 are selected from a hydrogen atom, C1-10 alkyl group, and the like, but R10 through R14 are not simultaneously hydrogen atoms; X is a halogen atom and the like; j and k are each either 0 or 1; and j+k is 0 or 2.

Abstract: The present application discloses complexes useful as catalysts for organic chemical synthesis including hydrogenation and dehydrogenation of unsaturated compounds or dehydrogenation of substrates. The range of hydrogenation substrate compounds includes esters, lactones, oils and fats, resulting in alcohols, diols, and triols as reaction products. The catalysts of current application can be used to catalyze a hydrogenation reaction under solvent free conditions. The present catalysts also allow the hydrogenation to proceed without added base, and it can be used in place of the conventional reduction methods employing hydrides of the main-group elements. Furthermore, the catalysts of the present application can catalyze a dehydrogenation reaction under homogenous and/or acceptorless conditions. As such, the catalysts provided herein can be useful in substantially reducing cost and improving the environmental profile of manufacturing processes for variety of chemicals.

Abstract: A diamine of formula (I) is described in which A is hydrogen or a saturated or unsaturated C1-C20 alkyl group or an aryl group; B is a substituted or unsubstituted C1-C20 alkyl, cycloalkyl, alkaryl, alkaryl or aryl group or an alkylamino group and at least one of X1, X2, Y1, Y2 or Z is a C1-C10 alkyl, cycloalkyl, alkaryl, aralkyl or alkoxy substituting group. The chiral diamine may be used to prepare catalysts suitable for use in transfer hydrogenation reactions.

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: Provided herein are stabilized radioiodinated and astatinated compounds, and to methods for their preparation.

Abstract: A new class of ligands derived from benzo[h]quinoline are described and these ligands are used to prepare several novel transition metal complexes. The complexes are preferably of the group VIII transition metals iron, ruthenium or osmium, with the benzo[h]quinoline ligands acting as tridentate ligands. The complexes described are proved to be very active catalysts for the reduction of ketones and aldehydes to alcohols, via hydrogen transfer and hydrogenation reactions. These compounds hence can be usefully employed as catalysts in said reduction reactions.

Abstract: Disclosed are a process and catalysts useful for carrying out asymmetric methlyallylations. The catalysts used in the invention have the formula (IV): wherein X1, X2, R3 and R4 are as defined herein. Compounds made by the process of the invention can be used to prepare pharmaceutically active compounds such as 11-?-hydroxysteroid hydrogenase type 1 (11-?-HSD1) inhibitors including 1,3-disubstituted oxazinan-2-ones.

Abstract: The present invention relates to a method for producing aryl-, heteroaryl- or alkenyl-substituted unsaturated hydrocarbons, containing: reacting aryl halides, heteroaryl halides or alkenyl halides with alkynes or alkenes in the presence of a palladium catalyst to obtain a crude product, and subsequently distillatively purifying the crude product in the presence of a compound having at least one NC?S group.

Abstract: A direct trifluoromethylation method preferably using a trifluoromethane as a fluoro-methylating species. In particular, the present method is used for preparing a trifluoromethylated substrate by reacting a fluoromethylatable substrate with a trifiuoromethylating agent in the presence of an alkoxide or metal salt of silazane under conditions sufficient to trifluoromethylate the substrate; wherein the fluoromethylatable substrate includes chlorosilanes, carbonyl compounds such as esters, aryl halides, aldehydes, ketones, chalcones, alkyl formates, alkyl halides, aryl halides, alkyl borates, carbon dioxide or sulfur.

Abstract: Described herein are fluorinated organic compounds and methods of making fluorinated organic compounds, for example, using palladium complexes. Also described herein are compositions and kits containing compounds and palladium complexes described herein.

Abstract: Provided is a ruthenium complex that is represented by general formula (1*) and is useful as an asymmetric reduction catalyst. (In the formula, * is an asymmetric carbon atom; R1 is an arenesulfonyl group, and the like; R2 and R3 are a phenyl group, and the like; R10 through R14 are selected from a hydrogen atom, C1-10 alkyl group, and the like, but R10 through R14 are not simultaneously hydrogen atoms; X is a halogen atom and the like; j and k are each either 0 or 1; and j+k is 0 or 2.

Abstract: A method for producing a fluorine-containing substituted compound, the method including: introducing an organofluorine compound and an organolithium compound into a microreactor provided with a flow path capable of mixing a plurality of liquids, to thereby obtain a reaction product; and introducing, into the microreactor, the reaction product and an electrophile exhibiting electrophilic effect on the reaction product, to thereby obtain a fluorine-containing substituted compound.

Abstract: A production method of a ?-fluoroalcohol includes performing a reaction of an ?-fluoroester with hydrogen gas (H2) in the presence of a specific ruthenium complex (i.e. a ruthenium complex of the general formula [2], preferably a ruthenium complex of the general formula [4]). This production method can employ a suitable hydrogen pressure of 1 MPa or less by the use of such a specific ruthenium complex and does not require a high-pressure gas production facility when put in industrial practice. In addition, this production method can remarkably reduce the amount of catalyst used therein (to e.g. a substrate/catalyst ratio of 20,000) in comparison to the substrate/catalyst ratio conventional reduction of ?-fluoroalcohol. It is possible by these reduction in hydrogen pressure and catalyst amount to largely reduce the production cost of the ?-fluoroalcohol.

Abstract: The present invention relates to a chiral spiro-pyridylamidophosphine ligand compound, synthesis method therefor and application thereof. The chiral spiro-pyridylamidophosphine compound is a compound having a structure of Formula (I), a racemate or optical isomer thereof, or a catalytically acceptable salt thereof, and is mainly characterized by having a chiral spiro-dihydro-indene skeleton in its structure. The chiral spiro-pyridylamidophosphine compound may be synthesized with optical active 7-diaryl/alkylphosphino-7?-amino-1,1?-spiro-dihydro-indene or substituted 7-diaryl/alkylphosphino-7?-amino-1,1?-spiro-dihydro-indene having a spiro-skeleton as chiral starting material. The chiral spiro-pyridylamidophosphine compound may be used as a chiral ligand in asymmetric hydrogenation of a carbonyl compound catalyzed by iridium, in which the reaction activity is very high, the amount of the catalyst may be 0.0001 mol %, and the enantioselectivity of the reaction is up to 99.9% ee.

Abstract: A method of forming a fluorinated molecular entity includes reacting in a reaction mixture an aromatic halide, copper, a fluoroalkyl group, and a ligand. The aromatic halide includes an aromatic group and a halogen substituent bonded to the aromatic group. The ligand includes at least one group-V donor selected from phosphorus and an amine. The overall molar ratio of copper to aromatic halide in the reaction mixture is from 0.2 to 3. The method further includes forming a fluoroalkylarene including the aromatic group and the fluoroalkyl group bonded to the aromatic group. A composition, which may be used in the method, consists essentially of copper, the fluoroalkyl group, and the ligand, where the molar ratio of copper to the fluoroalkyl group is approximately 1.

Abstract: Provided is a catalyst for asymmetric reduction, which can be produced by a convenient and safe production method, has a strong catalytic activity, and has excellent stereoselectivity. The present invention relates to a ruthenium complex represented by the following formula (1): wherein R1 represents an alkyl group or the like; Y represents a hydrogen atom; X represents a halogen atom or the like; j and k each represent 0 or 1; R2 and R3 each represent an alkyl group or the like; R11 to R19 each represent a hydrogen atom, an alkyl group or the like; Z represents oxygen or sulfur; n1 represents 1 or 2; and n2 represents an integer from 1 to 3, a method for producing the ruthenium complex, a catalyst for asymmetric reduction formed from the ruthenium complex, and methods for selectively producing an optically active alcohol and an optically active amine using the catalyst for asymmetric reduction.

Abstract: The invention relates to an asymmetric hydrogenation method for ketone compounds, comprising the step of: under hydrogen atmosphere, in the presence of an in situ catalyst derived from a chiral ligand and a ruthenium salt, adding a ketone compound and a base into a second solvent to carry out an asymmetric hydrogenation for the ketone compound. The invention can obtain a conversion of 100% and a highest asymmetric inducement effect of 99.7% for the ketone compound. The invention has the advantages including simple procedure, high conversion and selectivity, good atom economy and good prospect of industrial application.

Abstract: Disclosed are a novel, simple and low-cost method for preparing sitagliptin, as DPP-IV (dipeptidyl peptidase IV) inhibitor, which is useful in treating type 2 diabetes mellitus and key intermediates used in said preparation of sitagliptin.

Abstract: The present invention provides an organic metal compound, a ligand, an asymmetric catalyst, and a process for preparing optically-active alcohols using the asymmetric catalyst.

Abstract: Provided are a process for the preparation of phenyl carbamate derivatives, useful in the treatment of CNS (central nervous system) disorders, an intermediate in the synthesis of the phenyl carbamate derivatives, and a process for preparation of the intermediate.

Abstract: A substituted alkenylbenzene compound of formula (4): wherein X1 is a halogen atom, —SF5, C1-C6haloalkyl, hydroxy C1-C6haloalkyl, C1-C6alkoxy C1-C6haloalkyl, C3-C8halocycloalkyl, C1-C6haloalkoxy, C1-C3haloalkoxy C1-C3haloalkoxy, C1-C6haloalkylthio, C1-C6haloalkylsulfinyl or C1-C6haloalkylsulfonyl; X3 is a hydrogen, halogen, cyano, nitro, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy or C1-C6alkylthio; X4 is a hydrogen, halogen, cyano, C1-C4alkyl, C1-C4alkoxy or C1-C4haloalkoxy; R3 is —C(R3a)(R3b)R3c, where R3a and R3b are a halogen, or R3a and R3b together form a 3- to 6-membered ring together with the carbon bonding them by forming a C2-C5haloalkylene chain, and R3c is a hydrogen, halogen, C1-C5alkyl, C1-C5haloalkyl, C1-C4haloalkoxy or C1-C4haloalkylthio, with a proviso that where X1 is a fluorine, chlorine or trifluoromethyl, and X2 and X3 are hydrogen, where X1 and X2 are fluorine and X3 is a hydrogen, or where X1 and X2 are trifluoromethyl and X3 is a hydrogen, R3c is a hydrogen, chlorine, bromine, iodine,

Abstract: A tetrafluorotoluene compound represented by the formula (1): wherein R represents a C1-C6 alkyl group, and a method for producing a tetrafluorotoluene compound represented by the formula (1) which comprises hydrogenating a tetrafluorobenzyl alcohol compound represented by the formula (2): Wherein R represents a C1-C6 alkyl group.

Abstract: The present invention relates to a fluorine-containing cyclic compound of formula (5): wherein R2-R4 and R9-R15 are independently a hydrogen atom, a halogen atom, or a C1-C25 straight-chain, branched or cyclic alkyl group, and may contain fluorine atom, oxygen atom, sulfur atom, or nitrogen atom. R10 and R11, R12 and R13, or R14 and R15 may be bonded together to form a ring. In such a case, it is a C1-C25 alkylene group that may contain a hetero atom such as oxygen, sulfur and nitrogen, “a” is 0 or 1, “b” is an integer of 0-2 and “c” is an integer of 0-2.

Abstract: This invention concerns novel substituted unsaturated tetracyclic tetrahydrofuran derivatives with binding affinities towards serotonine receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in claim 1.

Abstract: A 2-fluoro-1,3-benzodithiol 1,1,3,3-tetraoxide derivative as a monofluoromethyl group introduction agent that is effective as an intermediate in pharmaceutical and agrochemical synthesis, a production method thereof, and a production method of a monofluoromethyl group-containing compound using this 2-fluoro-1,3-benzodithiol 1,1,3,3-tetraoxide derivative are provided. The 2-fluoro-1,3-benzodithiol 1,1,3,3-tetraoxide derivative represented by the following general formula (1) (wherein R1, R2, R3, and R4 each independently represent a hydrogen atom, a straight-chain or branched alkyl group having 1 to 4 carbon atoms, a straight-chain or branched alkyloxy group having 1 to 4 carbon atoms, a halogen atom, a nitro group, or a cyano group), the production method thereof, and various monofluoromethyl group-containing compounds are manufactured using this 2-fluoro-1,3-benzodithiol 1,1,3,3-tetraoxide derivative as a monofluoromethylating agent.

Abstract: The object of the present invention is to solve the problems in the prior arts, and to find more improved reaction conditions for suppressing the racemization of the product and obtaining an optically active alcohol at a high optical purity. The inventors achieved to solve the above problems by using a solvent system that is capable of resolving both an asymmetric catalyst and a formate salt, allowing the hydrogen source and the asymmetric catalyst to be present in the same phase.

Abstract: A process for producing 4-methyl-2,3,5,6-tetrafluorobenzyl alcohol including the following steps: (A): a step for fluorinating 2,3,5,6-tetrachloroterephthaloyl dichloride, (B): a step for reducing the product obtained in step (A), (C): a step for chlorinating the product obtained in step (B), and Step (D): a step for hydrogenating the product obtained in step (C).

Abstract: Chiral amino alcohol and amino phosphine compounds are provided herein, which compounds are useful for asymmetric synthesis.

Abstract: The invention relates to methods for carbon-carbon bond forming reactions, carbon-nitrogen bond forming reactions and/or carbon-oxygen bond forming reactions using phosphonium borate compounds represented by the Formula: (R1)(R2)(R3)PH.BAr4, wherein R1, R2, R3, and Ar4 are as defined herein in combination with a transition metal, transition metal salt, transition metal oxide or transition metal complex.

Abstract: The present invention relates to novel pesticidal azolidine derivatives as well as to oxazolidinone derivatives and their use as pesticides for combating animal parasites which occur in the agrochemical field and in the field of veterinary medicine, respectively. wherein X, m, R?, Q, G, U, l, A1 to A4 and R are as defined herein.

Abstract: The present invention relates to compounds useful as pharmaceutical intermediates, to processes for preparing the intermediates, to intermediates used in the processes, and to the use of the intermediates in the preparation of pharmaceuticals. In particular, the present invention concerns enantiomerically pure trans-cyclopropane carboxylic acid derivatives, processes for preparing the carboxylic acid derivatives and their use in preparing pharmaceuticals.

Abstract: The present invention relates to a process for preparing phenylalkan-1-ols in three stages, where an ester condensation in the presence of alkali metal or alkaline earth metal alcoholates is carried out in the first stage.

Abstract: A process for producing 4-methyl-2,3,5,6-tetrafluorobenzyl alcohol including the following steps: (A): a step for fluorinating 2,3,5,6-tetrachloroterephthaloyl dichloride, (B): a step for reducing the product obtained in step (A), (C): a step for chlorinating the product obtained in step (B), and Step (D): a step for hydrogenating the product obtained in step (C).

Abstract: Organic compounds having t-butyl ester or BOC carbonate protecting groups are effectively deprotected by heating in a fluorinated alcohol solution.

Abstract: The present disclosure includes catiome complexes of iron, ruthenium, and osmium, and their use as catalysts in organic synthesis transformations including the hydrogenation of unsaturated compounds. The complexes are represented by the following formulae I, II, III, IV, and V, wherein M is Fe, Ru or Os, P is a monodentate ligand with a phosphorus donor atom, P2 is a bidentate neutral ligand with two phosphorus donor atoms, N2 is a bidentate neutral ligand with two nitrogen donor atoms, PN is a bidentate neutral ligand with phosphorus and nitrogen donor atoms, PNNP is a tetradentate neutral ligand bonded to M via two phosphorus and two nitrogen atoms, X is any anionic ligand, LB is any neutral Lewis base, Y is any non-coordinating anion, n is 0, 1, or 2, m is 1 or 2, q is 0 or 1, r is 1 or 2 and q+r=2.

Abstract: The present invention relates to the field of catalytic hydrogenation and, more particularly, to the use of Ru complexes with bidentate ligands, having one amino or imino coordinating group and one phosphino coordinating group, in hydrogenation processes for the reduction of esters or lactones into the corresponding alcohol or diol respectively.

Abstract: The invention relates, in general, to an improved process for preparing compounds (e.g., 3-(3-trifluoromethylphenyl)propanal (Compound III, below)), which are key intermediates for the synthesis of cinacalcet, its salts and/or solvates thereof, as well as the use of such compounds prepared by such process for the preparation of cinacalcet and/or its salts or solvates.

Abstract: The present invention provides an organic metal compound, a ligand, an asymmetric catalyst, and a process for preparing optically-active alcohols using the asymmetric catalyst.

Abstract: A fluorine-containing benzaldehyde is reacted with an alkyl Grignard reagent to convert it to a magnesium alkoxide of racemic, fluorine-containing, benzyl alcohol, and subsequently the magnesium alkoxide is reacted with phthalic anhydride to obtain a phthalate half ester of racemic, fluorine-containing, benzyl alcohol, and the half ester is optically resolved by optically active 1-phenylethylamine, and then the ester group is hydrolyzed, thereby producing an optically active, fluorine-containing, benzyl alcohol.

Abstract: A process for the production of an alcohol compound represented by the formula (3): wherein X1, X2, X3, X4, Z, R and n are as defined below, comprising reacting a phenol represented by the formula (1): wherein X1, X2, X3 and X4 independently represent a hydrogen atom, a halogen atom or an alkyl group having 1 to 3 carbon atoms; Z represents an oxygen atom or a sulfur atom; and R represents an alkyl group, an alkenyl group, an alkynyl group, or an aralkyl group which may be substituted by a halogen atom, with a haloalcohol represented by the formula (2): wherein Y represents a chlorine atom or a bromine atom; and n represents an integer of 2 or 3, in a biphase system composed of a water-immiscible organic solvent and an aqueous alkali metal hydroxide solution in the presence of a phase-transfer catalyst.

Abstract: The present invention relates to, for example, a fluorine-containing cyclic compound represented by the following general formula (1). In the general formula (1), R1a is a C1-C25 cyclic alkyl group, cyclic alkenyl group or cyclic alkynyl group; each of R2 and R3 is independently a hydrogen atom, a halogen atom, or a C1-C25 straight-chain, branched or cyclic alkyl group; and each of R1a, R2 and R3 may contain fluorine atom, oxygen atom, sulfur atom, nitrogen atom or an atomic group containing a carbon-carbon double bond.

Abstract: The present invention relates to a process for lithium exchange reactions comprising mixing at least two fluids in a microreactor having at least two injection points.

Abstract: Vitamin D derivatives, notably non-steroidal vitamin D derivatives, are prepared from novel disubstituted phenylboronic acid compounds having the formula (I): and also from the novel intermediates having the formulae (1), (2), (3) and (10):

Abstract: The present invention relates to compounds of Formula I: wherein variable substituents are defined herein, that modulate the activity of or bind to chemokine receptors such as CCR5. In some embodiments, the compounds of the invention are selective for CCR5. The compounds can be used, for example, to treat diseases associated with chemokine receptor expression or activity such as inflammatory diseases, immune diseases and viral infections.

Abstract: A diamine of formula (I) is described, in which A is hydrogen or a saturated or unsaturated C1-C20 alkyl group or an aryl group; B is a substituted or unsubstituted C1-C20 alkyl, cycloalkyl, alkaryl, alkaryl or aryl group or an alkylamino group and at least one of X1, X2, Y1, Y2 or Z is a C1-C10 alkyl, cycloalkyl, alkaryl, aralkyl or alkoxy substituting group. The chiral diamine may be used to prepare catalysts suitable for use in transfer hydrogenation reactions.