Abstract: A method for production of hydroxycarboxylic acid amide compounds, including performing amide condensation between an ?- or ?-hydroxycarboxylic acid compound and an amine compound in the presence as a catalyst of an alkylboronic acid represented by R3B(OH)2 (wherein R3 is a primary alkyl group) or an arylboronic acid compound to produce a hydroxycarboxylic acid amide compound, the arylboronic acid compound being represented by Formula (1): (in Formula (1), —(CH2)nNR1R2 is bonded at an ortho position or a para position, n is 1 or 2, R1 is a tertiary alkyl group, R2 is a secondary or tertiary alkyl group, and —NR1R2 may be a ring).

Abstract: Disclosed is a method involving reacting a deprotonated mono- or dialkanol amine with one or more C4 to about C75 fatty acid monoalcohol esters.

Abstract: A compound of the formula R1.[(AO)n.—R2]m (I) where: R1 is the residue of a group having at least m active hydrogen atoms; AO is an alkylene oxide residue; each n is independently from 1 to 100; m is at least 2; and each R2 is independently H, a C1 to C21 hydrocarbyl, or an acyl group —OC.R3, where R3 is a C1 to C21 hydrocarbyl group, wherein on average greater than one of the R2 groups is or comprises a C4 to C21 hydrocarbyl group comprising at least two ethylenic double bonds. The compounds are particularly suitable for use in preparing aqueous emulsions or dispersions of resins and polymers, especially alkyd resins.

Abstract: The compounds of general formula (I) wherein: R1 is hydrogen, phenyl, C1-6 alkyl which can be further substituted with R3, R3 is 5- or 6-membered aromatic or heteroaromatic ring system which can be further substituted with benzyl or hydroxyl groups; R2 is OR4, NHR4, R4 is hydrogen, C1-6 alkyl or benzyl n is an integer from 1 to 12 or the salts of compounds mentioned which can form gels with commercial fuels, organic solvents and water.

Abstract: The present invention relates to a process for preparing substituted 2-aminobiphenyls and to a process for preparing (Het)arylamides of such 2-aminobiphenyls.

Abstract: A process for manufacturing dialkyl lactamide including reacting lactide and dialkylamine selected from one or more of dimethylamine, diethylamine, and methylethylamine to form a reaction mixture which includes dialkyl lactamide selected from N,N-dimethyl lactamide, N,N-diethyl lactamide, and N,N-methylethyl lactamide, N,N-dialkyl lactoyl lactamide, and dialkylamine, subjecting the reaction mixture to a separation step to form a product stream including N,N-dialkyl lactamide, a first recycle stream including dialkylamine and a second recycle stream including N,N-dialkyl lactoyl lactamide, feeding the recycle streams to the reaction step, and isolating the product stream. The process allows the manufacture of N,N-dimethyl lactamide, N,N-diethyl lactamide, and N,N-methylethyl lactamide on a commercial scale.

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: Disclosed is a method for preparing a compound of Formula 1 by contacting compound of Formula 2 with R1—NH2 in the presence of a carboxylic acid and a method for preparing a compound of Formula 2 by contacting a compound of Formula 4 with phosphorus tribromide. wherein R1 is H, C1-C4 alkyl, cyclopropyl, cyclopropylmethyl or methylcyclopropyl; R2 is CH3 or Cl; R3 is C1-C6 alkyl or C3-C6 alkenyl, each optionally substituted with up to 3 halogen and up to 1 phenyl; and X is Cl or Br. Also disclosed is a method for preparing a compound of Formula 5 wherein R4, R5, R6 and Z are as defined in the disclosure, using a compound of Formula 1 that is characterized by preparing the compound of Formula 1 by the method above.

Abstract: The present invention relates to a class of compounds and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds. More specifically the iodine containing compounds are chemical compounds containing an aliphatic central moiety containing urea or urethane functions allowing for the arrangement of three iodinated phenyl groups bound thereto. The invention also relates to the use of such diagnostic compositions as contrast agents in diagnostic imaging and in particular in X-ray imaging and to contrast media containing such compounds.

Abstract: A non-water soluble polymeric surfactant is prepared by reacting a polymerized/bodied unsaturated oil with maleic anhydride followed by a further partial or complete reaction with an amine to form an amide; or an alcohol to form an ester.

Abstract: A fluorine-containing polyether compound having the following general formula: (where R1 is a hydrogen atom, an alkyl group having 1 to 3 carbon atoms, or a phenyl group; X is a bromine atom or an iodine atom; l and m each are independently an integer of 10 or more; and l+m is 30-200) can be produced by reaction of a fluorine-containing dicarboxylic acid fluoride compound having the following general formula: (where l and m each are independently an integer of 10 or more, and l+m is 30-200) with an aromatic amine compound having the following general formula: [where R1 is a hydrogen atom, an alkyl group having 1 to 3 carbon atoms, or a phenyl group, R2 is a hydrogen atom or a group represented by the general formula —SiR3R4R5 (where R3, R4 and R5 each are independently an alkyl group having 1 to 10 carbon atoms or a phenyl group); and X is a bromine atom or an iodine atom] preferably in the presence of pyridine or a tertiary amine compound such as triethylamine, etc.

Abstract: the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n represents an integer being 1 or 2; R1 and R2 each independently represents hydrogen C1-4alkyl, NR9R10, C1-4alkyloxy; or R1 and R2 taken together with the carbon atom with which they are attached form a C3-6cycloalkyl; and where n is 2, either R1 or R2 may be absent to form an unsaturated bond; R3 represents a C6-12cycloalkyl, preferably selected from cylo-octanyl and cyclohexyl or R3 represents a monovalent radical having one of the following formulae ?wherein said C6-12cycloalkyl or monovalent radical may optionally be substituted with one, or where possible two, three or more substituents selected from the group consisting of C1-4alkyl, C1-4alkyloxy, halo or hydroxy; Q represents Het1 or Ar2 wherein said C3-8cycloalkyl, Het1 or Ar2 are optionally substituted with one or where possible two or more substituents selected from halo, C1-4alkyl, C1-4alkyloxy, hydroxy, nitro, NR5R

Abstract: An oxylamino group-containing compound represented by the following formula: R1—B-A-B—R2, wherein R1 represents a polymerizable group, R2 represents an oxylamino group-containing group or an oxylamino derivative-containing group, B represents an ester linkage or an amide linkage, and A represents an optionally substituted alkylene group having 2 to 12 carbon atoms.

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: A fluorine-containing polyether compound having the following general formula: (where R1 is a hydrogen atom, an alkyl group having 1 to 3 carbon atoms, or a phenyl group; X is a bromine atom or an iodine atom; l and m each are independently an integer of 10 or more; and l+m is 30-200) can be produced by reaction of a fluorine-containing dicarboxylic acid fluoride compound having the following general formula: (where l and m each are independently an integer of 10 or more, and l+m is 30-200) with an aromatic amine compound having the following general formula: [where R1 is a hydrogen atom, an alkyl group having 1 to 3 carbon atoms, or a phenyl group, R2 is a hydrogen atom or a group represented by the general formula —SiR3R4R5 (where R3, R4 and R5 each are independently an alkyl group having 1 to 10 carbon atoms or a phenyl group); and X is a bromine atom or an iodine atom] preferably in the presence of pyridine or a tertiary amine compound such as triethylamine, etc.

Abstract: A process for the production of ene-amide derivatives represented by the formula (I) wherein R1 and R2 and R3 are independently a hydrogen atom, an alkyl, a cycloalkyl, a cycloalkylalkyl, an alkylaryl, an aryl, a heterocycle, a cyano, an alkoxy, an aryloxy, a carboxyl, a carbamoyl, —CONR5R6 (in which R5 and R6 are independently an alkyl, arylalkyl or aryl group said ring being substituted or not with a functional group or with R5) or —COOR5 group (in which R5 is an alkyl, alkylaryl or aryl group), said alkyl, cycloalkyl, cycloalkylalkyl, alkylaryl and aryl groups being substituted or not with a functional group or with R5; or R1 and R2 taken together, may form a ring (which terms includes mono-, di- and higher polycyclic ring systems); R4 is a hydrogen atom, an alkyl, an aryl, an alkylaryl, said groups are substituted or not with a halogen atom as Cl, Br, or F; X is an oxygen atom or a leaving group and m is an integer 1 or 2; when m is 1 then X is a leaving group; when m is 2 then X is a oxygen atom, whi

Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.

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 compounds of general formula (I) wherein: R1 is hydrogen, phenyl, C1-6 alkyl which can be further substituted with R3, R3 is 5- or 6-membered aromatic or heteroaromatic ring system which can be further substituted with benzyl or hydroxyl groups; R2 is OR4, NHR4, R4 is hydrogen, C1-6 alkyl or benzyl n is an integer from 1 to 12 or the salts of compounds mentioned which can form gels with commercial fuels, organic solvents and water.

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: A method of producing a polymeric material including subjecting a starting material to conditions under which polymerisation occurs. The starting material includes a group of sub-formula (XIII) where R16 is selected from hydrogen, halo, nitro, hydrocarbyl, optionally substituted or interposed with functional groups, or R2 and R3 are independently selected from (CR6R7)n or a group CR8R9, CR6R7CR8R9 or CR8R9CR6R7 where n is 0, 1 or 2 and R6 and R7 are independently selected from hydrogen or alkyl, and either one of R8 or R9 is hydrogen and the other is an electron withdrawing group, or R8 or R9 together form an electron withdrawing group. R4 and R5 are independently selected from CH or CR1o where CR1o is an electron withdrawing group, X1 is a group CX2X3, Y1 is a group CY2Y3, and X2 X3, and, if present, Y2 and Y3, are each a C1 to C4 alkyl group.

Abstract: Methods for producing a compound of formula k1 or k2 by reducing a dihydronapthalene amide compound of formula i with hydrogen gas in the presence of a ruthenium catalyst of formula j1 or j2 Ru(Z)2(L)??j1; Ru(E)(E?)(L)(D)??j2; wherein m, n, Ar, Y, R1 E, E?, D, Z and L are as defined herein.

Abstract: Process for the industrial synthesis of the compound of formula (I)

Abstract: The present invention relates to a method for the preparation of Florfenicol from Fluoroamine compound, namely (1R,2S)-1-[4-(methylsulfonyl)phenyl]-2-amino-3-fluoro-1-propanol (II), by reaction with dihaloacetic acid ester in an organic solvent in presence of an inorganic base.

Abstract: The present invention relates to iodine containing compounds containing a central cyclopropane scaffolding moiety allowing for the arrangement of three iodinated phenyl groups bound thereto. The invention also relates to the use of such diagnostic compositions as contrast agents in diagnostic imaging and in particular in X-ray imaging and to contrast media containing such compounds.

Abstract: Provided is a process for preparing Cinacalcet, (R)-?-methyl-N-[3-[3-(trifluoromethyl)phenyl]propyl]-1-naphthalenemethane amine and intermediates thereof.

Abstract: the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n represents an integer being 1 or 2; R1 and R2 each independently represents hydrogen C1-4alkyl, NR9R10, C1-4alkyloxy; or R1 and R2 taken together with the carbon atom with which they are attached form a C3-6cycloalkyl; and where n is 2, either R1 or R2 may be absent to form an unsaturated bond; R3 represents a C6-12cycloalkyl, preferably selected from cylo-octanyl and cyclohexyl or R3 represents a monovalent radical having one of the following formulae wherein said C6-12cycloalkyl or monovalent radical may optionally be substituted with one, or where possible two, three or more substituents selected from the group consisting of C1-4alkyl, C1-4alkyloxy, halo or hydroxy; Q represents Het1 or Ar2 wherein said C3-8cycloalkyl, Het1 or Ar2 are optionally substituted with one or where possible two or more substituents selected from halo, C1-4alkyl, C1-4alkyloxy, hydroxy, nitro, NR5R6

Abstract: Processes for preparing amides of retinoic acid are disclosed. Intermediates useful in the preparation of amides of retinoic acid are also disclosed. In one version of the invention, fenretinide is produced via activation of retinoic acid (tretinoin) via its corresponding mixed anhydride or mixed carbonate followed by reaction of the activated intermediate with 4-aminophenol. Other amides of retinoic acid and isomers of retinoic acid, such as the 9-cis-form or 13-cis-form can also be made by this invention.

Abstract: One aspect of the present invention relates to methods for synthesizing milnacipran or congeners thereof. Another aspect of the present invention relates to asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof. The present invention also relates to methods for synthesizing intermediates useful in the non-asymmetric or asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof.

Abstract: Compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.

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: Novel compounds of general formula (I), are provided with inhibitory properties for the type B botulism toxin activity, along with methods for preparation thereof and corresponding pharmaceutical compositions.

Abstract: A new process for the production of dendritic trimesic acid triamides is described.

Abstract: A dihydroxy aromatic compound having a Formula (I), wherein R1 is a C6–C60 aromatic divalent functionality, R2 at each occurrence, can be the same or different and is independently at each occurrence selected from the group consisting of a cyano functionality, a nitro functionality, a halogen, an aliphatic functionality having 1 to 10 carbons, a cycloaliphatic functionality having 3 to 10 carbons and an aromatic functionality having 6 to 10 carbons, and “n” is an integer having a value of 0 to 4.

Abstract: Compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.

Abstract: An efficient, simple, high yielding, eco-friendly process for the manufacture of tosylates quaternary ammonium salts of cinnamidoalkylamines and/or benzamidoalkylamines (Formula I) has been described. These compounds are substantive UV-absorbers. They are useful in making fabric care products and personal care products. The scope of this methodology has been demonstrated by converting water soluble organic sunscreen quaternary halides to their corresponding tosylates of Formula VI.

Abstract: This invention relates to an improved synthesis of 5-(N-[(S)-N-{N,N-bis( 2-chloroethyl)amino}phenoxycarbonyl)-&ggr;-glutamyl]amino)isophthalic acid (also named ZD9063P), a prodrug used in Antibody Directed Enzyme Prodrug Therapy (ADEPT), a targeted cytotoxic cancer therapy. Another aspect of the invention comprises a compound of Formula (I) in which R1 and R2 are chloro, R3 is an alphamethylbenzylamine salt of carboxylic acid, (R4)n represents a benzyl protected 3,5-dicarboxylic acid and the asterisked chiral carbon in Formula (I) has S configuration, preferably in crystalline form.

Abstract: The invention relates to new alkoximinoacetic acid amides, a process for their preparation and their use as agents for combating pests.

Abstract: The present invention relates to an improved and industrially advantageous process for the preparation of N, N-dimethyl-3-(4-methyl)benzoyl propionamide, which compound is a key intermediate for the synthesis of zolpidem hemitartrate, a non-benzodiazepine hypnotic agent.

Abstract: The invention relates to a process for the preparation of &agr;-aminosubstituted carboxylic acid amide compounds and/or their salts comprising reacting a carboxylic acid amide of a primary amine with a nitrosylating agent in the presence of a base followed by hydrolysis to give a hydroxy imino derivative followed by hydrogenation and if necessary converting a base or acid of the &agr;-aminosubstituted carboxylic acid amide into one of its salts.

Abstract: The invention concerns polyalkoxylated superamides of the following formulae: [R1—CONR2—CH2CHR3—O—CHR4—CHR5O)m—(CH2CH2O)n]9 p(I); R1—CON—[CH2CHR3—O—(CHR4—CHR5O)m—(CH2CH2O)n—X]2, formulae wherein: R1 presents a C7-C22 hydrocarbon radical; R2, R3, represent a hydrogen or a C1-C4 hydrocarbon radical; R4, R5 represent a hydrogen or an alkyl radical comprising 1 to 2 carbon atoms, provided that one or more of said two radicals is a hydrogen; X represents a hydrogen, a C1-C6 hydrocarbon radical, a phosphate, carboxylate, sulphate, sulphonate group; m ranges between 0 and 20 exclusive; n ranges between 0 and 50 exclusive; p is equal to 1 or 2, depending on what X represents. The invention also conerns a method for obtaining said compounds and their use in particular as emulsifying agent for oils.

Abstract: The invention provides solid support synthetic methods for producing combinatorial libraries of modulators of LXRs. The combinatorial libraries thus produced are useful both as diagnostic indicators of LXR&agr; function and as pharmacologically active agents. The combinatorial libraries find particular use in the treatment of disease states associated with cholesterol metabolism, particularly atherosclerosis and hypercholesterolemia.

Abstract: A magnetic recording medium including a lubricant topcoat having increased bonding to the medium surface comprises an amphiphilic lubricant molecule having a hydrophilic central portion including a plurality of polar functional groups bound to the medium surface and a pair hydrophobic fluoroalkyl ether or perfluoroalkylether end portions at respective ends of the hydrophilic central portion and extending away from the medium surface.

Abstract: Targeted C2-symmetric and unsymmetric chemical libraries for use in protein and receptor homodimerization and heterodimerization are constructed by solution phase methodologies. Exemplary libraries are prepared in a 60 to 10 sub-library format by symmetrical coupling of the constructed fragments with a mixture of tethering dicarboxylic acids. In each step of the 3-step reaction sequence, the reactants, unreacted starting material, reagents and their byproducts were removed by simple liquid-liquid or liquid-solid extractions providing the desired intermediates and final libraries in multi-milligram quantities in high purities (≧90-100%) independent of the reaction yields and without deliberate reaction optimization. The synthesis of a second prototypical library employed the olefin metathesis reaction to join and combinatorially randomize the length of linker tether.

Abstract: Substantive UV absorbing organic-soluble quaternary salts of cinnamidoalkylamine are described. Hair, skin and fabric care compositions containing the compounds of formula I. wherein R1 is a substituent, selected from H, halo, —OH, —NH2, —NO2, —OCH3, —N(CH3)2, alkyl groups containing from 1 to 6 carbon atoms, alkoxy groups containing from 1 to 6 carbon atoms, alkylamino or N,N-dialkylamino groups containing from 1 to 6 carbon atoms; R2 is selected from hydrogen, alkyl group containing from 1 to 12 carbon atoms; R3 and R4 are independently selected from benzyl, alkyl group containing from 1 to 12 carbon atoms; n is an integer from 1 to 6; R5 is selected from an alkyl group containing from 8 to 22 carbon atoms; alkenyl groups containing from 8 to 22 carbon atoms; R7 is selected from bromo, chloro, nitro, methyl and ethyl groups.

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: The invention relates to a method for producing compounds of general formula (I), wherein R1 and R2, each time they occur and independently of each other, mean hydroxy, C1-6-alkyl, C1-6-alkoxy, halogen, phenyl or phenoxy; R3 means hydrogen or C1-6-alkyl; m is a whole number from 0 to 4; and n is a whole number from 0 to 5. According to said method, diketene is reacted with a N-phenyl-p-phenylenediamine of general formula (II), wherein R1, R2, R3, m and n have the meanings given above, in the presence of 3-40% acetic acid and at temperatures of 20 to 100° C., preferably 60 to 70° C. The invention also relates to the compounds (I) with R3=C1,6-alkyl and the enamines that can be obtained from these by reaction with ammonia, and their hydration products.

Abstract: A solid phase synthetic method for preparing arylretinamides is provided. The method comprises reacting hexachloroacetone with a solvent-suspended resin-bound triphenylphosphine to provide a suspension comprising an activated chlorinating reagent; reacting retinoic acid with the activated chlorinating reagent to provide retinoyl chloride; adding pyridine and a select arylamine to the resulting mixture; and stirring the resulting mixture for a time and at a temperature sufficient for the select arylamine to react with the retinoyl chloride and provide the arylretinamide. Also provided, are select arylretinamides that can be prepared by the present method, and methods of using such arylretinamides to induce apoptosis in cancer cells.

Abstract: The present invention provides intermediates of formula IIb and IIc useful for the preparation of Simvastatin: wherein R1 and R2 are each independently an alkyl, heteroalkyl, aryl or heteroaryl moiety, or R1 and R2, taken together, form a heterocyclic moiety containing 5-8 atoms; wherein each of the foregoing alkyl and heteroalkyl moieties may be linear or branched, substituted or unsubstituted, cyclic or acyclic or saturated or unsaturated, and each of the foregoing heterocyclic, aryl and heteroaryl moieties may be substituted or unsubstituted.

Abstract: The present invention is directed to an improved synthesis of clasto-lactacystin-&bgr;-lactone, and analogs thereof, that proceeds in fewer steps and in much greater overall yield than syntheses described in the prior art. The synthetic pathway relies upon a novel stereospecific synthesis of an oxazoline intermediate and a unique stereoselective addition of a formyl amide to the oxazoline. Also described are novel clasto-lactacystin-&bgr;-lactones, and analogs thereof and their use as proteosome inhibitors.