Abstract: A novel process for the preparation of N-methyl-N-(2-[4-hydroxyphenyl]ethyl)-5-hydroxy-4-methoxy benzene carboxamide, which is useful as an intermediate in the synthesis of (?)-galantamine, comprises the reaction of a 5-hydroxy-4-methoxy benzoic acid derivative with N-methyl-N-(2-[4-hydroxyphenyl]ethyl) amine.

Abstract: The present invention relates to a process for the preparation of threo-3,4-epoxy-2-amino-1-substituted butane derivatives represented by general Formula I which comprises reacting compound of Formula III or salt thereof with an active ester of acid of Formula IV and treating the product thereof with base. The carbon atom bonded to the radical R3 in Formula I and IV is in the (R)-, (S)- or (R,S)-configuration. The compounds of Formula I and III, particularly in their (2S,3R) configuration are useful intermediates for the preparation of atazanavir bisulfate.

Abstract: The invention relates to a continuous method for producing amides, according to which at least one carboxylic acid of formula (I) R3—COON ??(I) wherein R3 is hydrogen or an optionally substituted alkyl group comprising between 1 and 4 carbon atoms, is reacted with at least one amine of formula (II) HNR1R2 ??(II) wherein R1 and R2 are independently hydrogen or a hydrocarbon group comprising between 1 and 100 C atoms, to form an ammonium salt, and said ammonium salt is then reacted to form a carboxylic acid amide, under microwave irradiation in a reaction pipe, the longitudinal axis of the pipe being oriented in the direction of propagation of the microwaves of a monomode microwave applicator.

Abstract: Suggested is the use of amides and/or polyamides obtainable by condensation of (a) mono- and/or dicarboxylic acids and (b) amines and/or polyamines as auxiliary agents for aqueous asphalt and bitumen compositions.

Abstract: A process for reacting, in the presence of a particular calcium containing catalyst, an amine having an active hydrogen and one or more of a fatty acid ester or a fatty acid.

Abstract: The present invention relates to an improved process for the preparation of the active pharmaceutical ingredient, vorinostat. In particular it relates to an efficient process for the preparation of vorinostat of high purity without the requirement to isolate any synthetic intermediate compounds.

Abstract: The invention provides methods of treating Friedreich's ataxia using histone deacetylase inhibitors.

Abstract: A method for producing a diamine includes purifying a diamine from an aqueous solution containing a diamine salt by adding an alkaline substance to the aqueous solution and then filtering the resulting solution by allowing the solution to pass through a nanofiltration membrane to remove the salt, thereby obtaining an aqueous diamine solution.

Abstract: The present invention generally relates to processes for the chemocatalytic conversion of a carbohydrate source to an adipic acid product. The present invention includes processes for the conversion of a carbohydrate source to an adipic acid product via a furanic substrate, such as 2,5-furandicarboxylic acid or derivatives thereof. The present invention also includes processes for producing an adipic acid product comprising the catalytic hydrogenation of a furanic substrate to produce a tetrahydrofuranic substrate and the catalytic hydrodeoxygenation of at least a portion of the tetrahydrofuranic substrate to an adipic acid product. The present invention also includes products produced from adipic acid product and processes for the production thereof from such adipic acid product.

Abstract: The present invention relates to a process for producing an aliphatic carboxylic acid amide, including the step of reacting an aliphatic carboxylic acid or an alkyl ester thereof containing an alkyl group having 1 to 4 carbon atoms with a mono- or dialkylamine containing an alkyl group or groups having 1 to 4 carbon atoms in the presence of a solid acid catalyst containing titanium oxide as a main component and an oxide or oxides of at least one element selected from elements (except titanium) belonging to Groups 4, 5 and 14 of the long form of the periodic table, wherein the catalyst has an average particle diameter of 2 ?m or more. The process for producing an aliphatic carboxylic acid amide according to the present invention has a high reaction efficiency of the reaction of the aliphatic carboxylic acid or alkyl ester thereof with the mono- or dialkylamine, and shows an excellent filtration efficiency in separation of the catalyst.

Abstract: Disclosed herein is a method for chemically attaching carboxyl, alcohol, amine or amide groups to the surface of nanodiamond (ND) in a liquid phase. Also disclosed herein are a functional ND compound obtained by the method and use thereof. The method includes treating synthetic ND with a size of 1 nm-1OO nm with sonication and a strong acid to provide ND-(COOH)n. The ND-(COOH)n compound is used as a starting material to provide ND compounds having alcohol, amine or amide groups attached to the surfaces thereof. The surface-functionalized ND compounds are characterized by using an X-ray diffractometer, FTIR, AFM, particle size analyzer and zeta sizer. The ND compounds show functionalities as well as high solubility to provide stable ND solutions in a liquid phase. Therefore, the ND compounds may be used as diamond coating agents. The powder of the ND compounds may be used as materials for producing composites of polymers, plastics, synthetic fibers, ceramics, etc.

Abstract: This object relates to a natural leather which is obtained by forming a coating film through the greasing step following re-tanning and dyeing and the drying step. The purpose of this object is to provide a natural leather, wherein the generation of free formaldehyde and acetaldehyde is inhibited, and a treating agent to be added in the greasing step for natural leather. A natural leather wherein formaldehyde and acetaldehyde generated by a tanning agent, a re-tanning agent, a dye and a greasing agent having been incorporated into a leather are confined in the leather with a treating agent to be added in the greasing step for natural leather which contains a hydrazide compound optionally together with sodium hydrogen sulfite to thereby inhibit or prevent the generation of formaldehyde and acetaldehyde, and an automobile interior part coated with this natural leather.

Abstract: The present invention relates to a process for the preparation of gabapentin and, more in particular, to a method of synthesis of 1,1-cyclohexane acetic acid monoamide, an intermediate used in the preparation of gabapentin, comprising the basic hydrolysis reaction of ?, -diaminocarbonyl-?,?-pentamethylene glutarimide.

Abstract: Fluoroalkyl amidoalkyl alcohols of the formula are disclosed and their corresponding (meth)acrylate esters. These fluoroalkyl amidoalkyl (meth)acrylate monomers can be copolymerized with a wide variety of conventional ethylenically unsaturated monomers. The resulting copolymers are useful as water, oil- and grease-proofing agents for paper, textiles and hard surfaces such as masonry and wood.

Abstract: Disclosed are, for example, a process for producing a tricarboxylic acid tris(alkyl-substituted cyclohexylamide), the process comprising subjecting a tricarboxylic acid and an alkyl-substituted cyclohexylamine to an amidation reaction, either (a) in the presence of a boric acid compound and a phenol compound or (b) in the presence of a boric acid ester obtained by the dehydration condensation of a boric acid compound and a phenol compound, and optionally purifying the resulting crude reaction product.

Abstract: According to one aspect of the present invention there is provided a substantially high purity D-(?)-N,N-diethyl-2-(?-naphthoxy)propionamide and a process for the manufacture of substantially higher purity D-(?)-N,N-diethyl-2-(?-naphthoxy)propionamide having chemical purity near about or above 95%, and chiral purity near about or more than 97%. According to another aspect of the invention is to provide an agrochemical compositions containing highly pure optically active D-(?)-N,N-diethyl-2-(?-naphthoxy)propionamide.

Abstract: A process for preparing N,N-dimethylacetamide (DMAC) by continuously reacting methyl acetate (MeOAc) with dimethylamine (DMA) in the presence of a basic catalyst, wherein MeOAc is used in the form of a methanolic solution and the continuous distillative workup is effected in such a way that methanol and any other low boilers are initially removed overhead in a column A and the bottom effluent of column A is fed to a column B in which DMAC is removed via a side draw a purity of ?99.7% by weight.

Abstract: The invention relates to a method for the continuous production of alkyl amino acryl amides by reacting alkyl acrylates with high-boiling amines. A specific preparation technique is used in order to achieve hitherto unobtainable product qualities. Very high spatial, temporal and overall yields can also be obtained.

Abstract: The invention provides compounds of formula (I) wherein R1 represents hydrogen or alkyl; R2 represents an unsubstituted or substituted heterocycle or R2 represents an unsubstituted or substituted aryl; R3 represents alkyl or halogen; X represents a single bond or an alkandiyl-group, optionally interrupted by one or more oxygen atoms or carbonyl groups or carbonyloxy groups in free base or acid addition salt form, processes for their preparation and their use as pharmaceuticals.

Abstract: Chemotherapeutic conjugates of a peptide substrate to a phosphoramide chemotherapeutic agent in which a peptide substrate is covalently linked to the chemotherapeutic agent by a linker with an aminoarylmethyl or aminoheteroaryl moiety, wherein the linking of the peptide to the chemotherapeutic agent inhibits the cytotoxic activity of the chemotherapeutic agent, the peptide is a substrate for proteolytic cleavage by a tumor-specific enzyme; and the linker is capable of undergoing 1,6-elimination in vivo upon cleavage of the peptide substrate. Methods for synthesizing and methods of using the conjugates are also disclosed.

Abstract: An amide is formed by reacting an ?-ketoacid or salt thereof in a decarboxylative condensation reaction with an amine or salt thereof comprising a nitrogen covalently bound to an atom selected from oxygen, nitrogen, and sulfur. The amide bond is formed between the ?-carbon of the ketoacid and the nitrogen of the amine. The ?-ketoacid can be formed using a novel sulfur reagent.

Abstract: The invention relates to a process for continuously preparing alkylamino(meth)acrylamide by reacting methyl (meth)acrylate, ethyl (meth)acrylate or amines having a high boiling point compared to methanol or ethanol. A special workup technique which includes removing water from the amine before entering the reactor allows product qualities which have hitherto not been attained to be achieved. In addition, very high space-time and overall yields can be achieved.

Abstract: The invention encompasses processes for the synthesis of (S)-(+)-3-(aminomethyl)-5-methylhexanoic acid, (S)-Pregabalin, and intermediates of (S)-Pregabalin.

Abstract: Disclosed are, for example, a process for producing a tricarboxylic acid tris(alkyl-substituted cyclohexylamide), the process comprising subjecting a tricarboxylic acid and an alkyl-substituted cyclohexylamine to an amidation reaction, either (a) in the presence of a boric acid compound and a phenol compound or (b) in the presence of a boric acid ester obtained by the dehydration condensation of a boric acid compound and a phenol compound, and optionally purifying the resulting crude reaction product.

Abstract: Novel cyclohexyl-1,4-diamine compounds corresponding to formula I, processes for the production thereof, pharmaceutical compositions containing these compounds, methods of producing pharmaceutical compositions including these compounds and related methods of treating or inhibiting certain diseases or conditions.

Abstract: Compounds of formula (I) wherein R1 to R4, X and A are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as tissue-selective androgen receptor modulators (SARM) and are useful in hormonal therapy, e.g., in the treatment or prevention of male hypogonadism and age-related conditions such as andropause.

Abstract: A process for preparing N,N-dimethylacetamide (DMAC) by continuously reacting methyl acetate (MeOAc) with dimethylamine (DMA) in the presence of a basic catalyst, wherein MeOAc is used in the form of a methanolic solution and in the range from 0.0002 to 0.09 mol of catalyst per mole of MeOAc, and performing the reaction at a temperature in the range from 90 to 140° C. and at an absolute pressure in the range from 10 to 30 bar.

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 composition comprises a condensation product of an amine-reactive fluorinated polyether and a polyamine. The compositions may be in dispersed in water.

Abstract: A water-stable and water-soluble ceramic precursor is provided, containing at least one Group III element. Also, a metal acid salt complex is provided comprising (1) bismuth, lanthanum, and titanium, and (2) a polyether acid. In addition, methods are provided for preparing the Group III metal acid salt complex and the Bi, La, Ti acid salt complex comprising a bismuth polyether acid salt complex, a lanthanum polyether acid salt complex, and a titanium polyether acid salt complex. Finally, devices that include lanthanum-doped bismuth titanate as the active component are provided, as well as a water-stable and water-soluble gallium polyether acid complex.

Abstract: The invention relates to 4-propargyloxy-benzyl dervatives of the general formula (I) including the optical isomers thereof and mixtures of such isomers, wherein R1 is hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl or optionally substituted aryl; R2, R3, R5, R6, and R7 are each independently of each other hydrogen or optionally substituted alkyl; R4 is optionally substituted alkyl; X is O or N—R7; and R8 is a group R9 is optionally substituted aryl or optionally substituted heteroaryl; R10 and R11 are each independently hydrogen, optionally substituted alkyl, optionally substituted alkenyl or optionally substituted alkynyl; R12 is optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl or optionally substituted heteroaryl; R13 is hydrogen or optionally substituted alkyl, alkenyl or alkynyl; and R14 is optionally substituted alkyl or optionally substituted amino.

Abstract: A method of treating ocular hypotension, hypertension, hemorrhage, myocardial ischemia, angina pectoris, coronary contraction, cerebrovascular contraction after subarachnoidal hemorrhage, cerebral hemorrhage and asthma which comprises administering to a mammal suffering therefrom a therapeutically effective amount of a thromboxane ligand which is a compound formula I, wherein Y is (CH2)x; Z is selected from the group consisting of and (CR2)x, x is an integer of 1 or 2; n is 0 or 1; R2 is hydrogen or an alkyl radical of from 1 to 4 carbons; A is an alkylene or alkenylene radical having from two to seven carbon atoms, which radical may be substituted with one or more hydroxy, oxo, alkyloxy or alkylcarboxy groups or said alkylene or alkenylene may have one or more enchained oxa or imino radicals; B is a methyl radical or a cycloalkyl radical having from three to seven carbon atoms, or an aryl radical, selected from the group consisting of hydrocarbyl aryl and heteroaryl radicals wherein the heteroatom is

Abstract: The present invention relates to a synthetic process for the preparation of a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor.

Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, X, W, m and n are as defined hereinabove. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, parasite infections, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.

Abstract: The use of compounds of formula (I), and salts thereof; and pharmaceutically acceptable in vivo cleavable prodrugs of said compound of formula (I); and pharmaceutically acceptable salts of said compound or said prodrugs; in formula (I), Ring C is phenyl or a carbon linked heteroaryl ring substituted as defined within; R1 is an ortho substituent as defined within; n is 1 or 2; A-B is a linking group as defined within; R2 and R3 are as defined within; R4 is hydroxy, hydrogen, halo, amino or methyl; in the manufacture of a medicament for use in the elevation of PDH activity in warm-blooded animals such as humans is described.

Abstract: Disclosed is a process for preparing a tetra-amide which comprises carrying out a condensation reaction between a diacid, a monoacid, and a diisocyanate, thereby forming a tetra-amide. Also disclosed is a process for preparing a phase change ink composition which comprises (a) carrying out a condensation reaction between a diacid, a monoacid, and a diisocyanate, thereby forming a tetra-amide; and (b) admixing the tetra-amide thus formed with a colorant, thereby forming a phase change ink.

Abstract: The invention relates to 3-phenyl-propionamido, 3-phenyl-acrylamido and 3-phenyl-propynamido derivatives, for example, deriviatives of the formula wherein A is selected from R1, R3, R4, R5, R6, R7, R21, R22, R23, R24, and n are as defined herein or pharmaceutically acceptable salts thereof. The invention also relates to processes for preparation of such compounds, compositions containing them, and the use of such derivatives as MAO-B inhibitors. The invention further relates to methods for treating or preventing Alzheimer's disease and senile dementia by administering compounds of the invention.

Abstract: The invention relates to novel pesticidally active ?-sulfin- and ?-sulfonamino acid amides of the general formula (I) including the optical isomers thereof and mixtures of such isomers, wherein n is a number zero or one, R1-R7 have the meanings given in the specification. R8 is either hydrogen, (a), (b), (c), (d) or (e) wherein R11, R12, R14, R15 and R17 are each independently hydrogen or C1-C4alkyl, R13 is C4-C12alkyl; C1-C12 halogenalkyl; C3-C8 cycloalkyl; optionally substituted aryl or optionally substituted heteroaryl, R16 is optionally substituted aryl or optionally substituted heteroaryl; and Z is oxygen, sulfur —CR18R19— or —NR20—, wherein R18, R19, R20 independently of each other are hydrogen or C1-C4alkyl.

Abstract: Compounds, in particular those based on polyisobutyleneamines, are suitable as emulsifiers for water-in-oil emulsions and are used in particular as additives for fuels and lubricants.

Abstract: Synthetic methods and compounds involving amino amides, peptides and peptidomimetics. Amino amide derivatives are prepared via the one-step three-component reaction of a glyoxamide, an amine, and an organoboron derivative. Conversion of the product to another glyoxamide intermediate allows the iterative use of this chemistry for the synthesis of peptides and peptidomimetics.

Abstract: The invention relates to a method for producing amides or esters from carboxylic acids and from an amine constituent or alcohol constituent in the presence of a 1,3,5-triazine and optionally in the presence of an organic solvent and of a tertiary amine. According to the invention, a (bi)cyclic diamine or an adduct formed therefrom with the triazine constituent is used as a tertiary amine in a preferred stoichiometric ratio of diamine to the triazine constituent ranging from 0.30 to 1.10; the stoichiometric ratio of carboxylic acid to the amine constituent or alcohol constituent should range from 0.2 to 5.0, and; the molar ratio of carboxylic acid to the triazine constituent ranges from 0.5 to 1.5. Amino acids such as N-protected amino acids and peptides serve as carboxylic acid constituents and (C-protected) amino acids or a C-protected peptide serve as the amine constituent.

Abstract: Compounds of the formula R2.[(AO)n.R3]m, where R2 is a residue of a group having at least m active hydrogen atoms derived from hydroxyl and/or amino and/or amido groups, AO is alkyleneoxy, n is 2 to 200; R3 includes residue(s) of alkenyl succinic acids and optionally other acids, and m is 2 to 10, but when m is 2 there are other restrictions in the definitions, are disclosed as useful thickeners and/or dispersants in aqueous systems. The use of such materials as thickeners is also disclosed.

Abstract: Novel perfluoroalkyl-substituted mono-, di- and poly-amide compounds which are reaction products of a mono-, di- or polyamine of 60 to 2000 molecular weight with a perfluoroalkyl substituted unsaturated acid or its corresponding lower alkyl ester and optionally a non-fluorinated amino-reactive compound such as an acid, ester, anhydride, epichlorohydrin, isocyanate or urea, are useful as internally or externally applied paper sizes to impart oil and grease resistance to paper, and as oil proofing coatings on textiles, wood, masonry and the like, or as high-performance surface active agents.

Abstract: The present invention relates to the formation of an amido ester having the formula: R1—CO—NR3—R2—COL or R1—NR3—CO—R2—COL wherein R1 is C1-C12 linear or branched alkyl, C6-C14 aryl, C7-C14 alkyl substituted aryl unit; R2 is C1-C14 alkylene, C6-C14 arylene, C7-C14 alkyl substituted arylene; R3 is hydrogen, C1-C10 alkyl, C6-C10 aryl, C7-C10 alkyl substituted aryl, L is a aryl leaving group having the formula: R4 comprises one or more anionic or cationic units, wherein said compound is formed using a spinning disc reactor.

Abstract: This invention relates to fluorophenyl-substituted alkenylcarboxylic acid guanidides, process for their preparation, their use as a medicament or diagnostic, and medicament containing them. An embodiment of the invention embraces compounds of the formula I: and the pharmaceutically tolerated salts thereof. The disclosed compounds are valuable inhibitors of the cellular sodium/proton exchanger (Na+ /H+ exchanger) . They are therefore outstandingly suitable for the treatment of all diseases attributable to increased Na+ /H+ exchange.

Abstract: The invention concerns the use of amide derivatives of formula (I) wherein: R1 and R2 are substituents such as hydroxy, C1-6alkoxy, mercapto, C1-6alkylthio, amino, C1-6alkylamino and di-(C1-6alkyl)amino; m and p are independently 0-3R3 is C1-4alkyl; q is 0-4; and R4 is aryl or cycloalkyl; or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for use in the treatment of diseases or medical conditions mediated by cytokines

Abstract: The use of compounds of the formula (I), and salts thereof; and pharmaceutically acceptable in vivo cleavable prodrugs of said compound of formula (I); and pharmaceutically acceptable salts of said compound or said prodrugs: wherein: Ring C is phenyl or a carbon linked heteroaryl ring substituted as defmed within; R1 is an ortho substituent as defined within; n is 1 or 2; A—B is a linking group as defined within; R2 and R3 are as defined within; R4 is hydroxy, hydrogen, halo, amino or methyl; in the manufacture of a medicament for use in the elevation of PDH activity in warm-blooded animals such as humans is described. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are also described.

Abstract: This invention employs camphorsultam as a chiral recoverable auxiliary to provide a new method for manufacturing valproic acid and valproic acid amides that facilitates the enantioselective or diasteroselective production of valproic acid analogs on a larger scale.

Abstract: A method of preparing carboxylic acid derivatives comprising mixing a quaternary ammonium salt having a particular triazine ring in the molecules thereof, a carboxylic acid compound and a compound having a nucleophilic functional group, to condense the carboxylic acid with the compound having the nucleophilic functional group. The invention further provides a condensing agent comprising the quaternary ammonium salt. The condensation is conducted under mild conditions to form carboxylic acid derivatives and, particularly, amide compounds or ester compounds maintaining high yields.

Abstract: The invention provides a process for the production of a condensation product selected from the group consisting of an amide and an ester of a carboxylic acid from an organic compound selected from the group consisting of organic compounds carrying a hydroxyl group and organic compounds carrying an amine group and from a concentrated medium resulting from fermentation, said medium containing a salt of the acid, the salt being selected from the group consisting of a sodium salt, a calcium salt, and mixtures thereof and the medium being at a pH of at least the pKa of the acid, the process comprising reacting the medium with the organic compound and with CO2, whereby the condensation product and a salt selected from the group consisting of sodium carbonate, sodium bicarbonate, calcium carbonate, calcium bicarbonate, and mixtures thereof are formed; and, separating the condensation product from the reaction mixture formed in the previous step.