Abstract: Aspects of the present disclosure include conformationally restricted analogs of catecholamine type compounds (e.g., isoprenaline, adrenaline, noradrenaline) which activate ?2AR with high selectivity over ?1AR. The subject beta-2 selective adrenergic receptor agonist compounds may serve as bronchiodilators and find use in the treatment of a variety of bronchoconstrictive diseases and conditions. Also provided are compositions and methods for treating preterm labor. A method of treating acute asthma including administration of a subject compound to a subject in need thereof is provided. The subject method can provide for reduced undesirable side effects associated with non-selective ?-adrenergic receptor agonism, such as inotropic and chronotropic effects that leads to elevated blood pressure. The compounds can also be used to prevent or treat heart failure. Kits and compositions for practicing the subject methods are also provided.

Abstract: Disclosed herein is a method for producing an alcohol and an amine from an amide under an atmosphere of hydrogen with the use of, as a catalyst, a ruthenium complex that is easily prepared, easy to handle, and relatively cheaply obtained. Specifically, the method is a method for producing an alcohol and/or an amine from an amide compound under an atmosphere of hydrogen with the use of as a catalyst, a ruthenium carbonyl complex represented by the following general formula (1): RuXY(CO)(L) (1) wherein X and Y may be the same or different from each other and each represents an anionic ligand and L represents a tridentate aminodiphosphine ligand containing two phosphino groups and a —NH— group.

Abstract: Disclosed is a method for producing a compound having an amino group and/or a hydroxyl group from a substrate compound having an atomic group containing CO or CS by eliminating such atomic group. The substrate compound, having an atomic group containing CO or CS (for example, an amide, a carbamate, or the like), is allowed to react with a compound expressed by formula (I) below, at a temperature of 120° C. or lower, preferably in the presence of an ammonium salt, to eliminate such atomic group containing CO or CS. In formula (I) A may not be present, and in a case where A is present, A represents an alkyl group having 1 to 6 carbon atoms. H2N-A—NH2 (I) - - -.

Abstract: The invention relates to a process for the production of radiotracers. In particular, this invention relates the isolation of radiotracers with containers filled with a stationary phase.

Abstract: We have developed a new method for the synthesis of Rasagiline (Formula 1) based on the alkylation of trifluoroacetyl protected aminoindan. This protection enabled us to carry out an alkylation of aminoindan with a high yield and purity under very mild conditions with a wide range of reaction conditions and reagent selection. Considering the ease, purity and high yields of introducing and removal of the trifluoroacetyl group, this approach is a highly practical and economical way for the synthesis of rasagiline or its pharmaceutically acceptable salts.

Abstract: Provided is a method for preparing 4,4?-dinitrodiphenylamine (4,4?-DNDPA) in high yield via the NASH reaction using a mixture of a bis-quaternary ammonium base and a base catalyst for the reaction of urea with nitrobenzene, and a method of preparing 4,4?-bis(alkylamino)diphenylamine (4,4?BAADA) in high yield and purity by hydrogenating the resulting 4,4?-DNDPA with a ketone in the presence of hydrogen and hydrogenation catalyst. The catalyst complex used in the present invention allows easy recovery, provides superior alkaline stability and is capable of reducing production cost.

Abstract: Provided is a method of preparing 4,4?-dinitrodiphenylamine (4,4?-DNDPA) in high yield by reacting 4-nitroaniline with excess nitrobenzene via the NASH reaction, and a method of preparing 4,4?-bis(alkylamino)diphenylamine (4,4?BAADA) in high yield and purity by hydrogenating the resulting 4,4?-DNDPA with a ketone compound in the presence of hydrogen and hydrogenation catalyst. The disclosed process is simple, allows selective preparation of 4,4?-DNDPA without byproducts, and thus allows preparation of 4,4?-BAADA in high yield without a complicated purification procedure.

Abstract: There is provided a process for the reduction of one or more amide moieties in a compound comprising contacting the compound with hydrogen gas and a transition metal catalyst in the presence or absence of a base under conditions for the reduction an amide bond. The presently described processes can be performed at low catalyst loading using relatively mild temperature and pressures, and optionally, in the presence or absence of a base or high catalyst loadings using low temperatures and pressures and high loadings of base to effect dynamic kinetic resolution of achiral amides.

Abstract: This invention provides a convenient method for converting oximes into enamides. The process does not require the use of metallic reagents. Accordingly, it produces the desired compounds without the concomitant production of a large volume of metallic waste. The enamides are useful precursors to amides and amines. The invention provides a process to convert a prochiral enamide into the corresponding chiral amide. In an exemplary process, a chiral amino center is introduced during hydrogenation through the use of a chiral hydrogenation catalyst. In selected embodiments, the invention provides methods of preparing amides and amines that include the 1,2,3,4-tetrahydro-N-alkyl-1-naphthalenamine or 1,2,3,4-tetrahydro-1-naphthalenamine substructure.

Abstract: The present invention relates to a (2R, 3R)-3-(3-substituted phenyl)-2-methyl n-pentanamide compounds as shown in the formula I and the preparation method thereof, wherein, the substituents are as defined in the specification, the present invention further relates to a use of the above compounds for the preparation of tapentadol II or its pharmaceutically acceptable salt, and the intermediates involved in the preparation process.

Abstract: We have developed a new method for the synthesis of Rasagiline (Formula 1) based on the alkylation of trifluoroacetyl protected aminoindan. This protection enabled us to carry out an alkylation of aminoindan with a high yield and purity under very mild conditions with a wide range of reaction conditions and reagent selection. Considering the ease, purity and high yields of introducing and removal of the trifluoroacetyl group, this approach is a highly practical and economical way for the synthesis of rasagiline or its pharmaceutically acceptable salts.

Abstract: The present invention relates to novel Ruthenium catalysts and related borohydride complexes, and the use of such catalysts, inter alia, for (1) hydrogenation of amides (including polyamides) to alcohols and amines; (2) preparing amides from alcohols with amines (including the preparation of polyamides (e.g., polypeptides) by reacting dialcohols and diamines and/or by polymerization of amino alcohols); (3) hydrogenation of esters to alcohols (including hydrogenation of cyclic esters (lactones) or cyclic di-esters (di-lactones) or polyesters); (4) hydrogenation of organic carbonates (including polycarbonates) to alcohols and hydrogenation of carbamates (including polycarbamates) or urea derivatives to alcohols and amines; (5) dehydrogenative coupling of alcohols to esters; (6) hydrogenation of secondary alcohols to ketones; (7) amidation of esters (i.e.

Abstract: Disclosed herein is a method for producing an alcohol and an amine from an amide under an atmosphere of hydrogen with the use of, as a catalyst, a ruthenium complex that is easily prepared, easy to handle, and relatively cheaply obtained. Specifically, the method is a method for producing an alcohol and/or an amine from an amide compound under an atmosphere of hydrogen with the use of as a catalyst, a ruthenium carbonyl complex represented by the following general formula (1): RuXY(CO)(L) (1) wherein X and Y may be the same or different from each other and each represents an anionic ligand and L represents a tridentate aminodiphosphine ligand containing two phosphino groups and a —NH— group.

Abstract: The present invention provides processes and intermediates for the preparation of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine and salts thereof which are useful as serotonin-2C (5-HT2C) receptor agonists for the treatment of, for example, obesity.

Abstract: The invention relates to a method for removing an alkyl sulfonyl or aryl sulfonyl protecting group from a primary or secondary amine by contacting an alkyl sulfonamide or an aryl sulfonamide with a Stage 0 or Stage I alkali metal-silica gel material in the presence of a solid proton source under conditions sufficient to form the corresponding amine. The invention also relates to a method for removing an alkyl sulfonyl or aryl sulfonyl protecting group from a primary or secondary amine by a) reacting an alkyl sulfonamide or an aryl sulfonamide with a Stage 0 or Stage I alkali metal-silica gel material, and b) subsequently reacting the reaction product from step a) with an electrophile or a proton source. Preferred Stage 0 or Stage I alkali metal-silica gel materials include Na, K2Na, and Na2K.

Abstract: The invention relates to a process for the production of radiotracers. In particular, this invention relates the isolation of radiotracers with containers filled with a stationary phase.

Abstract: Provided is a method of preparing 4,4?-dinitrodiphenylamine (4,4?-DNDPA) in high yield by reacting 4-nitroaniline with excess nitrobenzene via the NASH reaction, and a method of preparing 4,4?-bis(alkylamino)diphenylamine (4,4?BAADA) in high yield and purity by hydrogenating the resulting 4,4?-DNDPA with a ketone compound in the presence of hydrogen and hydrogenation catalyst. The disclosed process is simple, allows selective preparation of 4,4?-DNDPA without byproducts, and thus allows preparation of 4,4?-BAADA in high yield without a complicated purification procedure.

Abstract: Provided is a method for preparing 4,4?-dinitrodiphenylamine (4,4?-DNDPA) in high yield via the NASH reaction using a mixture of a bis-quaternary ammonium base and a base catalyst for the reaction of urea with nitrobenzene, and a method of preparing 4,4?-bis(alkylamino)diphenylamine (4,4?BAADA) in high yield and purity by hydrogenating the resulting 4,4?-DNDPA with a ketone in the presence of hydrogen and hydrogenation catalyst. The catalyst complex used in the present invention allows easy recovery, provides superior alkaline stability and is capable of reducing production cost.

Abstract: The present invention relates to processes for preparing enantiomerically pure cyclopropyl amine derivatives and salts thereof; the chiral intermediates such as the chiral salts are useful for the preparation of such chiral compounds and salts; pharmaceutical compositions comprising the compounds and salts; and method of using such compositions. The chiral cyclopropyl amine derivatives are useful for binding to histamine H3 receptor sites and for providing therapeutic agents for histamine H3 mediated disease.

Abstract: A process for the preparation of substituted 1-aminomethyl-2-phenyl-cyclohexane compounds.

Abstract: This invention provides alignment materials for liquid crystal display device of vertical alignment mode and methods for the preparation of the same, and more particularly, it provides diaminobenzene derivatives represented by the following formula 1 (shown in description), capable of aligning liquid crystal in uniform and vertical way and remarkably improving clarity and solubility against organic solvents, methods for the preparation of the same and liquid crystal alignment films using the same.

Abstract: The invention relates to novel compounds of formula I where R1, R2, R3, R4, R5, R9, Ar, Q1, Q2 and Q3 are each as defined below. The compounds of the formula I have antithrombotic activity and inhibit especially protease-activated receptor 1 (PAR1). The invention further relates to a process for preparing the compound of the formula I and to the use thereof as a medicament.

Abstract: There are provided a 4-(trichloromethylthio)aniline represented by the general formula (II): wherein R1 represents a hydrogen atom or an alkyl group having 1 to 3 carbon atoms, R2 each independently represents a halogen atom, an alkyl group having 1 to 3 carbon atoms, or a perfluoroalkyl group having 1 to 3 carbon atoms, R3 represents a formyl group, an acetyl group, or a trifluoroacetyl group, and m represents an integer of 0 to 4, a method for producing the same, and a method for producing a 4-(trifluoromethylthio)aniline derivative using the 4-(trichloromethylthio)aniline. It becomes possible to produce a 4-(trifluoromethylthio)aniline with a high yield by using raw materials that can easily be obtained industrially and using general purpose production facilities.

Abstract: The present invention provides processes and intermediates for the preparation of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine and salts thereof which are useful as serotonin-2C (5-HT2C) receptor agonists for the treatment of, for example, obesity.

Abstract: A hyperdispersant for use in a fluorocarbon coating composition is disclosed. The fluorocarbon coating composition generally comprises a fluorocarbon resin, a binder resin, a cross-linking agent, and the hyperdispersant. The hyperdispersant comprises the reaction product of a polyglycidyl oligomer and at least one amino compound. The polyglycidyl oligomer comprises a carbon chain having from 1 to 25 carbon atoms with at least one of an internal ether linkage and an internal ester linkage and comprises a plurality of epoxy groups. The at least one amino compound has a cyclic, heterocyclic, alkyl, or heteroalkyl structure substituted with at least one primary or secondary amine group for reacting with and opening at least one of the epoxy groups.

Abstract: Alkylated antioxidant macromolecules are represented by Structural Formula 1: wherein the variables are described herein. Also included are methods of making the molecules and methods of using the molecules as antioxidants.

Abstract: Provided is a one-step efficient production method for an ?,?-difluoroamine of a general formula (1) below from an amide compound. The method is an economical method capable of producing the intended ?,?-difluoroamine at high yield by reacting a starting amide compound with carbonyl fluoride and/or oxalyl fluoride under a specific condition.

Abstract: The present invention relates to a process for the preparation of (2S,3S)-3-amino-N-cyclopropyl-2-hydroxyalkanamides as well as novel compounds prepared or used in the process.

Abstract: Disclosed are 2-quinoxalinol salen compounds and in particular 2-quinoxalinol salen Schiff-base ligands. The disclosed 2-quinoxalinol salen compounds may be utilized as ligands for forming complexes with cations, and further, the formed complexes may be utilized as catalysts for oxidation reactions. The disclosed 2-quinoxalinol salen compounds also may be conjugated to solid supports and utilized in methods for selective solid-phase extraction or detection of cations.

Abstract: The present invention relates to a method of preparing optically active amines and chiral amines prepared thereby. The method includes reacting an amine compound, a metal catalyst, a biocatalyst including a lipase, and an acyl donor compound in an organic solvent to obtain a chiral amide compound, and then hydrolyzing the chiral amide compound to obtain a chiral amine.

Abstract: A method of decomposing a polycarbonate with water in a supercritical or subcritical state. A high-purity dihydroxy compound which is a constituent component of the polycarbonate can be recovered at a high yield by this decomposition method. This decomposition method is environment-friendly because it does not use an organic solvent, easy to be carried out, has a high decomposition rate and rarely causes a side reaction.

Abstract: Organic compounds having nitrogen atoms protected with t-butoxycarbonyl are effectively deprotected by heating in a fluorinated alcohol solution.

Abstract: This invention provides a convenient method for converting oximes into enamides. The process does not require the use of metallic reagents. Accordingly, it produces the desired compounds without the concomitant production of a large volume of metallic waste. The enamides are useful precursors to amides and amines. The invention provides a process to convert a prochiral enamide into the corresponding chiral amide. In an exemplary process, a chiral amino center is introduced during hydrogenation through the use of a chiral hydrogenation catalyst. In selected embodiments, the invention provides methods of preparing amides and amines that include the 1,2,3,4-tetrahydro-N-alkyl-1-naphthalenamine or 1,2,3,4-tetrahydro-1-naphthalenamine substructure.

Abstract: A process for synthesis of R-(?)-N,?-Dimethylphenethylamine (Levmetamfetamine, formula I), or S-(+)-N,?-Dimethyl phenethylamine (Methamphetamine, formula II), from d-ephedrine of formula III or l-ephedrine formula IV, the process comprising the steps of (a) acylating the d- or l-ephedrine base of formula III or formula IV with an acylating agent to make a reaction mixture containing a N-acylated ephedrines of formula V or formula VI; (b) deoxygenation of N-acylated ephedrines to make the compound of the formula VII or Formula VIII by using Raney Nickel catalyst; and (c) acid hydrolysis of the above deoxygenated products to get the levmetamfetamine or methamphetamine.

Abstract: A process for the preparation of optically active substituted alpha-amino-indane derivatives of formula (I), which include: an asymmetric hydrogenation reaction of an en-amide derivative of formula (III) in presence of hydrogen and an optically active catalyst, in order to obtain an amide derivative of formula (II), a hydrolysis reaction of the amide derivative of formula (II) obtained in the previous step, in order to obtain optically active substituted alpha-amino-indane derivatives of formula (I).

Abstract: A process for preparing a compound of formula I wherein R1 is H, C1-6alkyl, C2-6alkenyl, C1-6alkoxy, —OH, or amino; and n, m, and p are independently selected from 0, 1 and 2; which process comprises reacting a compound of formula II, by combining it with a reducing agent in a suitable solvent into a reaction mixture.

Abstract: The invention relates to a process for preparing arylamines or heteroarylamines or arylamides or heteroarylamides by cross-coupling of primary or secondary amines or amides with substituted aryl or heteroaryl compounds in the presence of a Brønsted base and a catalyst or precatalyst, wherein the catalyst comprises a) a transition metal, a complex, a salt or a compound of this transition metal selected from the group consisting of Ni, Pd and b) at least one ligand selected from the group consisting of bidentate bis(phosphino)alkanediyls having the following formula in a solvent or solvent mixture, where the radicals Ar1-4 are each, independently of one another, an aryl or heteroaryl substituent selected from the group consisting of phenyl, naphthyl, pyridyl and biphenyl or Ar1-4 is hydrogen, C1-, C2-alkyl, straight-chain, branched or cyclic C3-C8-alkyl, and L is an alkanediyl bridge which has from 1 to 20 carbon atoms.

Abstract: Provided is a method of preparing an optically pure compound having formula 1 or its salts. The method includes: reacting (R)-2-(4-methoxy-3-aminosulfonyl-phenyl)-1 -methylethylamine or its salts with a compound selected from the group consisting of chloroacetic acid, bromoacetic acid, fluoroacetic acid, iodoacetic acid, ?-halogenoacetic acid anhydride, and ?-halogenoacetyl halide in the presence of a base or an acylating agent.

Abstract: A process for the preparation of 4-hydroxyalkylamino-2-nitro-anisoles of the general formula (I) wherein m is 2 or 3; by reaction of a 4-halogeno-3-nitro-aniline of formula (II) with a chloroalkyl-chloroformate of formula (III), alkaline ring closure of the resulting carbamate and nucleophilic replacement of the halogeno atom by a methoxy group to form a derivative of formula (IV), and finally ring opening of the resulting cyclic carbamate by treatment with methanolic alkali metal hydroxide, followed by neutralization with inorganic or organic acids, wherein the complete reaction is executed in a non-aqueous medium; as well as process for the preparation of 2-amino-4-hydroxyalkylamino-anisoles of formula (V).

Abstract: The invention relates to a special two-step method for producing amines on the basis of amides by reacting them with halides or hypohalites in an aqueous solution in a Hofmann degradation reaction. The amide is reacted in an alkaline solution and/or suspension with halides or hypohalites and the reaction mixture obtained in step 1 is added to an aqueous alkaline solution having a temperature of at least 40° C.

Abstract: This invention describes the reaction of an alpha fluoroalkyl ketone with a bis(trialkylsilyl)amide to give a stable N-trialkylsilyl imine. Treatment of the N-trialkylsilyl imine with an alcohol leads to solvolysis of the trialkylsilyl group and yields a stable mixture of an aminal and an imine in high yield. Catalytic reduction of this mixture, or of the individual components, in the presence of a chiral catalyst leads to a fluoroalkyl amine with high enantioselectivity and high yield.

Abstract: A process for preparing 5,6-diethyl-2,3-dihydro-1H-inden-2-amine and acid addition salts thereof from 2-aminoindan. The process comprises protecting the amino group of 2-aminoindan, acetylating the ring in the protected compound, reducing the acetyl group to ethyl to form a monoethyl derivative, acetylating the monoethyl derivative, reducing the acetyl group to form a diethyl derivative, deprotecting the latter by hydrolysis and recovering the product in free or salt form. The process does not use deleterious Grignard reagents or nitrites such as isoamyl nitrite, and provides high regioselectivity and high yield of 5,6-diethyl-2,3-dihydro-1H-inden-2-amine. In addition, the process uses acetyl halide as both a reactant and a solvent.

Abstract: Disclosed is a method of preparing a composition comprising a compound represented Structural Formula (I): The method comprises the step of reacting an aldehyde compound R10CHO with an isonitrile compound represented by Structural Formula (II):

Abstract: The present invention relates to a silver halide color photographic light-sensitive material wherein at least one of light-sensitive silver halide emulsion layers includes a silver halide emulsion having a silver chloride content of at least 95 mol % and a silver iodide content of 0.05 mol % to 0.75 mol % and/or a silver bromide content of 0.05 mol % to 4.

Abstract: The present invention relates to a method of preparation for compounds of Formula 23: wherein R3, R4, R5, R6, R7, and W are as defined herein.

Abstract: Disclosed is a process for the preparation of amines by continuously feeding a carboxamide, aqueous alkaline hypohalite, and aqueous alkaline hydroxide to a first reaction zone to form a N-halocarboxamide, measuring the concentration of at least one reaction component in the effluent from the first reaction zone, and using the result of that measurement to control the feed rate of at least one of the feed components of to achieve at least 90% conversion of the carboxamide in the first reaction zone. The effluent from the first reaction zone is fed continuously to a second reaction zone where it further reacts to form an aqueous solution of an amine. The effluent from the second reaction zone may be fed continuously to a distillation column. The process is particularly useful for the preparation of cyclopropylamine.

Abstract: A process for working up distillation residues from the synthesis of tolylene diisocyanate by reaction of the distillation residues with water comprises reacting the TDI distillation residues with water in a continuous or semicontinuous process in a backmixed reactor in the presence of hydrolysate.

Abstract: In the process of the present invention, xylylenediamine and/or cyanobenzylamine is produced by a catalytic liquid-phase hydrogenation of a phthalonitrile compound. The liquid-phase hydrogenation is performed by controlling the concentration of a benzamide compound to a specific level or lower. In a preferred embodiment, the concentration of a benzoic acid compound is further controlled to a specific level or lower. By the process, xylylenediamine and/or cyanobenzylamine is produced at high yields and the catalyst life is prolonged.

Abstract: A process for preparing 6-hydroxy-3,4-dihydroquinolinone by intramolecular Friedel-Crafts alkylation of N-(4-methoxyphenyl)-3-chloropropionamide in which an equivalent of N-(4-methoxyphenyl)-3-chloropropionamide is contacted with a Lewis acid in DMSO or a high boiling amide or amine at an elevated temperature of from about 150° C. to about 220° C. is provided. The process produces 6-HQ in high yield and a high state of purity such that it may be used in subsequent reactions toward the preparation of cilostazol without intermediate purification. A process for preparing cilostazol from 6-hydroxy-3,4-dihydroquinolinone prepared by the process and improved processes for preparing N-(4-methoxyphenyl)-3-chloropropionamide are also provided.

Abstract: Bicyclic amino alcohols, whose amino group and hydroxy group are bonded in positions 1,3 adjacent to the bridge, for example are valuable ligands for metal complexes of the d-8 metals of the periodic table of elements. The metal complexes in question are catalysts or catalyst precursors for the asymmetric hydrogenation or asymmetric transfer hydrogenation with hydrogen donors of prochiral organic compounds with carbon double bonds or carbon/hetero atom double bonds, for example ketones and imines.