Abstract: The present invention relates to ethane-1,2-diaminium bis[(2R)-2-bromo-3-phenyl-propanoate], the preparation of ethane-1,2-diaminium bis[(2R)-2-bromo-3-phenyl-propanoate] from (2R)-2-bromo-3-phenylpropionic acid and ethylenediamine in 2-propanol, and the use of ethane-1,2-diaminium bis[(2R)-2-bromo-3-phenyl-propanoate] for the preparation of ACE/NEP inhibitors.

Abstract: The present invention relates to a 3-substituted-phenyl-3-merthylbutyric acid and 3-substituted-phenyl-3-merthylaldehyde derivatives, which are useful in the production of N-[N-[3-(3-hydroxy-4-methoxyphenyl)-3-methylbutyl]-L-?-aspartyl]-L-phenylalanine 1-methyl ester, which is a sweetener with high sweetening potency.

Abstract: A process for the preparation of meta or para-substituted &agr;-arylalkanoic acids of formula (I) wherein R and R1 are as defined in the disclosure.

Abstract: The present invention relates to new compounds of the formula (I) in which X represents alkyl, Y represents halogen or alkyl and Z represents halogen or alkyl, with the proviso that one of the radicals Y and Z always represents halogen and the other alkyl, Het represents one of the groups in which A, B, D and G have the meanings given in the description, a plurality of processes for their preparation and their use as pesticides and herbicides.

Abstract: An optically active amino acid derivative is produced by N-protecting an optically active 3-haloalanine derivative followed by cyclization, or cyclizing this derivative followed by N-protection to thereby give an optically active N-protected-aziridine-2-carboxylic acid derivative which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent, or by N-protecting an optically active 3-haloalanine derivative to thereby give N-protected-aziridine-2-carboxylic acid which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent. According to this process, natural and unnatural optically active amino acids can be produced from inexpensive materials by using simple procedures.

Abstract: Compounds represented by formula (1), wherein X is, for example, CH, CH2, CHR (wherein R is a lower alkyl group or a substituted lower alkyl group) or CRR′ (wherein R and R′ are the same as the above defined R); Y is, for example, CH, CH2 or C═O; Z is, for example, O, S, S═O or SO2; U is C or N; R1 to R4 are each independently, for example, a hydrogen atom, OR, SR (wherein R is the same as defined above), or an aromatic ring, a substituted aromatic ring or a heterocycle; at least one of R5 and R8 is, for example, OH and the remaining of R5 and R8 are each independently, for example, a hydrogen atom or OH, optical isomers thereof, conjugates thereof or pharmaceutically acceptable salts thereof are provided.

Abstract: This invention relates to novel compounds of the formula: wherein R1 is H or C1-C6alkyl and the C1-C6alkyl moiety is straight or branched; R2 and R3 are each independently C1-C6alkyl and the C1-C6alkyl moiety is straight or branched; X is Cl, Br or I; or stereoisomers thereof.

Abstract: The present invention relates to ethane-1,2-diaminium bis[(2R)-2-bromo-3-phenyl-propanoate], the preparation of ethane-1,2-diaminium bis[(2R)-2-bromo-3-phenyl-propanoate] from (2R)-2-bromo-3-phenylpropionic acid and ethylenediamine in 2-propanol, and the use of ethane-1,2-diaminium bis[(2R)-2-bromo-3-phenyl-propanoate] for the preparation of ACE/NEP inhibitors.

Abstract: The present invention relates to new cinnamic acid salts of salmeterol, processes for the preparation thereof as well as the use thereof as pharmaceutical compositions.

Abstract: 1 Compounds of formula (I), wherein R1 and R2 are, independently of one another, H, C1-C6alkyl, C1-C6halogenalkyl, C1-C6alkoxy, C1-C6alkoxy-C1-C6alkyl, or C1-C6alkoxy-C1l-C6alkyloxy, and R3 is C1-C6alkyl, are obtainable in high yields by stereoselective addition of R3-substituted propionic acid esters to R1- and R2-substituted benzaldehydes of formula R—CHO to form corresponding 3-R-3-hydroxy-2-R3-propionic acid esters, conversion of the OH group to a leavaing group, subsequent regioselective elimination to form 3-R-2-R3-propenic acid esters, and their hydrolysis to form corresponding propenic carboxylic acids and their enantioselective hydrogenation, wherein R is (a).

Abstract: A method for synthesizing compounds of Formula I in which R is alkyl or aryl and X is any halogen is described.

Abstract: The present invention is a process for the preparation of a compound of formula The compounds of formula I are valuable intermediates for the manufacture of therapeutically active compounds.

Abstract: The present invention relates to new compounds of the formula (I) in which X represents alkyl, Y represents halogen or alkyl and Z represents halogen or alkyl, with the proviso that one of the radicals Y and Z always represents halogen and the other alkyl, Het represents one of the groups  in which A, B, D and G have the meanings given in the description, a plurality of processes for their preparation and their use as pesticides and herbicides.

Abstract: Novel 2-substituted 7-haloindenes and methods for synthesizing such indenes are described. The 2-substituted 7-haloindenes may be coupled with any aryl group to produce a metallocene catalyst intermediate.

Abstract: An efficient and selective process, capable of scale-up, to make itaconate derivatives of formula (IV), and/or succinate derivatives of formula (V) and/or (VI) by asymmetric hydrogenation of the itaconate derivatives. wherein R, R1 and R2 are as defined herein.

Abstract: The present invention provides a compound of formula I or pharmaceutical acceptable salts thereof wherein R1 is C4-12 alkyl, C4-12 alkenyl, C4-12 alkynyl, —(CH2)h—C3-8 cycloalkyl, substituted and unsubstituted —(CH2)h-aryl, substituted and unsubstituted —(CH2)h-het, R2 is substituted and unsubstituted C1-12 alkyl, substituted and unsubstituted C2-12 alkenyl, substituted and unsubstituted C2-12 alkynyl, substituted and unsubstituted —(CH2)h—C3-8 cycloalkyl, substituted and unsubstituted —(CH2)h—C3-8 cycloalkenyl, substituted and unsubstituted —(CH2)h-aryl, substituted and unsubstituted —(CH2)h-heterocyclic ring, substituted and unsubstituted —(CH2)i—X—R4 (X is —O—, —S(═O)j—, —NR7—, —S(═O)2NR8—, or —C(═O)—), and —(CH2)iCHR5R6. The compounds are inhibitors of matrix metalloproteinases involved in tissue degradation.

Abstract: The present invention pertains to a process for the preparation of an enantiomerically enriched chiral carboxylic acid derivative having the partial formula: C—C—C—COOX wherein X is a cation, comprising formation of a dehydro precursor salt having the partial formula: C═C—C—COOX by reaction of the corresponding precursor acid with an at least substantially stoichiometric amount of base, and asymmetric hydrogenation of the salt in the presence of a transition metal complex of a chiral phosphine ligand.

Abstract: A method for preparing chloromethylphenylacetic acids represented by formula (II): wherein a methylphenylacetic acid represented by formula (I): is reacted with a chlorine gas, in an inert solvent, under the irradiation with light or in the presence of a radical initiator, is disclosed. According to the preparation method, high purity chloromethylphenylacetic acids can be prepared at a high yield, without using toxic sulfuryl chloride as a chlorinating agent, by chlorinating the methyl group of the methylphenylacetic acids at a high selectivity while suppressing by-production of a dichloro form or &agr;-chloro form.

Abstract: A process for preparing phenylacetic acid derivatives of the formula (I) by reacting benzyl chlorides of the formula (II) 1

Abstract: A method of synthesizing compounds of Formula I: by reacting aromatic compounds with butyrolactone, followed by neutralization with base. The reaction can be conducted in the presence of a catalyst. Preferred catalysts are Lewis acids. A preferred product of Formula I is 4-phenylbutyric acid, which is obtained by the reaction of benzene with butyrolactone in the presence of aluminum chloride, followed by neutralization with base.

Abstract: The present invention relates to a novel process for the preparation of aromatic carbonyl compounds by oxidative cleavage of styrenes using lipases and hydrogen peroxide or hydrogen peroxide donors in the presence of carboxylic acids or carboxylic esters.

Abstract: A description is given of new chiral phosphine ligands containing amino acid groups and having the formula I where R1 is hydrogen, a C1-C7-alkyl radical, a C6-C10-aryl radical or a monovalent metal, preferably sodium or potassium, R2 is hydrogen or a C1-C7-alkyl radical, R3 is hydrogen or an —NR5R6 radical, where R5 and R6 are identical or different and are hydrogen or C1-C7-alkyl or C6-C10-aryl radicals, m is 0 or 1, with the exception of the compounds in which R5 and R6 are hydrogen and at the same time R2 is hydrogen, R4 is phenyl and R1 is methyl or benzyl and a process for their preparation. These phosphine ligands are suitable as constituents of metal complexes which can be used as catalysts for reactions to form C—C, C—H, C—N, C—Si or C═O bonds.

Abstract: A process for obtaining &agr;,&agr;-dimethylphenylacetic acid wherein &agr;,&agr;dimethylbenzyl cyanide is reacted in the presence of sodium hydroxide, water and a C4- and/or C5-alcohol at temperatures above about 100° C. and the &agr;,&agr;-dimethylphenylacetic acid is obtained by acidification.

Abstract: The invention pertains to chiral ferrocene phosphine derivatives and their use with transition metals as asymmetric catalysts in asymmetric hydrogenation.

Abstract: It is described a process for preparing (R)-2-bromo-3-phenyl-propionic acid starting from (D)-phenyl-alanine, sodium nitrite and concentrated hydrobromic acid in a mixture of an aqueous solvent and a solvent selected from the group consisting of halogenated hydrocarbons and aromatic hydrocarbons.

Abstract: Palladium-catalyzed arylation of an olefin (e.g., ethylene) with an aromatic halide (e.g., 2-bromo-6-methoxynaphthalene, m-bromobenzophenone, or 4-isobutyl-1-bromobenzene) is conducted in specified media. After a special acid or base phase separation procedure, palladium-catalyzed carbonylation of the olefinically-substituted aromatic intermediate is conducted in specified media using CO and water or an alcohol to form arylalkylcarboxylic acid or ester or substituted arylalkylcarboxylic acid or ester (e.g., racemic 2-(6-methoxy-2-naphthyl)propionic acid, 2-(3-benzoylphenyl)propionic acid, or 2-(4-isobutylphenyl)propionic acid). Catalyst recovery procedures enabling recycle of catalyst residues and efficient recovery of amine hydrogen halide scavenger and solvent used in the arylation reaction are described, as well as novel, highly efficient methods of conducting the carbonylation reaction.

Abstract: A compound of the following formula ##STR1## wherein M is an alkali metal or alkaline earth metal atom and a process for the preparation of the compound is provided.

Abstract: The present invention relates to a process for the production of benzene derivatives represented by formula (I), which are useful as intermediates for agricultural chemicals, fine chemical products or pharmaceuticals such as anti inflammatory analgesics. The process includes reacting a compound of chemical formula (II) with a hydroformylating agent and a halogenating agent.

Abstract: The phenylalkan(en)oic acids of the formula: ##STR1## as defined herein, posses an antagonistic activity on leukotriene B.sub.4.

Abstract: Described herein is a novel process to resolve a racemic compound into its optically active isomers without need for chemical transformation such as salt formation. The process advantageously utilizes polymers containing chiral moieties in their repeat units as well as exhibiting critical solution temperature behavior in a suitable solvent. An embodiment describes the resolution of tryptophan.

Abstract: A process for preparing salts of pharmaceutical active substances which have acidic groups by reacting the carboxylic acids with a base in the melt, wherein the acids are reacted with at least the stoichiometric amount of a base in an extruder.

Abstract: The invention relates to a process for the preparation of 2-(pyrid-2-yloxymethyl)phenylacetates of formula (I) useful as intermediates for agricultural pesticides, which comprises reacting a 2-pyridine of formula (II), wherein L is a leaving group and A, D and m are as defined in the description with a compound MO--CH.sub.2 R where M is a metal atom and R is the residue of a metal salt of phenylacetic acid. It also includes the compounds MO--CH.sub.2 R, a process for their preparation and a "one-pot" process for the preparation of 2-(pyrid-2-yloxymethyl) phenylacetates from 3-isochromanone.

Abstract: This invention relates to a process for preparing carboxylic acids by oxidizing an aldehyde with a peracid in the presence of an amine and/or amine N-oxide catalyst selected from the group consisting of a substituted or unsubstituted alkyl amine, alkyl amine N-oxide, aromatic amine, aromatic amine N-oxide, heterocyclic amine, heterocyclic amine N-oxide and mixtures thereof, to produce the carboxylic acid. Such carboxylic acids have utility for example as chemical intermediates.

Abstract: Described herein is a novel process to resolve a racemic compound into its optically active isomers without need for chemical transformation such as salt formation. The process advantageously utilizes polymers containing chiral moieties in their repeat units as well as exhibiting critical solution temperature behavior in a suitable solvent. An embodiment describes the resolution of tryptophan.

Abstract: Supported phase catalysts in which the support phase, is non-aqueous and highly polar, such as a primary alcohol, and most preferably ethylene glycol, are. disclosed. An organometallic compound, preferably a metal complex of chiral sulfonated 2,2'-bis(diphenylphosphino)-1,1'-binaphthyl is dissolved in the ethylene glycol. Such supported phase catalysts are useful for asymmetric synthesis of optically active compounds, such as the preparation of dehydronaproxen.

Abstract: Description here is a novel process for preparing phenyl acetic acid derivatives of the formula (I)Ar--CH.sub.2 --R.sup.1 (I)in which Ar and R.sup.1 are as defined in the description by reaction of sulfonyloxy-activated hydroxyacetic acid derivatives of the formula (II)R.sup.3 --SO.sub.2 --O--CH.sub.r --R.sup.1 (II)in which R.sup.3 is as defined in the description. with aromatics of the formula (III)Ar--H (III)has been found. The intermediates of the formula (II), some of which are novel, are obtained from hydroxyacetic acid derivatives by reaction with sulfonyl halides or sulfonic anhydrides. The phenylacetic acid derivatives are important starting materials for preparing pesticides.

Abstract: A process for the preparation of aromatic substituted carboxylic acids is disclosed. The process comprisesi) forming an aromatic-substituted acrylonitrile by dehydrating a cyanohydrin of the formula ##STR1## where Ar is C.sub.6 to C.sub.10 aryl unsubstituted or substituted with C.sub.1 to C.sub.6 linear or branched alkyl, C.sub.1 to C.sub.6 linear or branched alkoxy, halo, amino, amino mono- or disubstituted with C.sub.1 to C.sub.6 linear or branched alkyl or carboxylic acid or the alkyl esters thereof; and R is hydrogen or C.sub.1 to C.sub.6 linear or branched alkyl;ii) catalytically reducing the aromatic-substituted acrylonitrile when not more than 10% of the cyanohydrin is converted to said acrylonitrile to form a first reaction solution comprising an aromatic substituted aliphatic nitrile;iii) hydrolyzing the aromatic-substituted aliphatic nitrile.

Abstract: Novel acetylsalicylic acid derivatives having general formula (I) are provided, in which R.sup.1 is hydrogen or methyl; R.sup.2 is --O-- or --NH--; and W is hydroxy, halogen, lower alkoxy, lower alkenyloxy, lower alkynyloxy, cycloalkyloxy, aryloxy, aralkyloxy, acyloxy, or --N(R.sup.3)(R.sup.4) wherein the lower alkoxy, the lower alkenyloxy, the lower alkynyloxy, the cycloalkyloxy, the aryloxy, the aralkyloxy, and the acyloxy are optionally substituted with hydroxy, carboxyl, lower alkoxy, lower alkyl, halogen, nitro, and amino. The invention also pertains to a polymer made from such derivatives and a medical equipment containing the polymer. The polymer is useful in the prevention of platelet aggregation thereon.

Abstract: Process for preparing 3-(p-fluorophenyl)-2-methylpropionic acid and derivatives thereof of the formula (I), ##STR1## in which R is a hydroxy group, a linear or branched (C.sub.1 -C.sub.8)-alkoxy group, an aryloxygroup, an amino group or a (C.sub.1 -C.sub.8)-alkylamino group or a (C.sub.1 -C.sub.8)-dialkylamino group, bya) converting p-fluoroaniline into the p-fluorophenyldiazonium salt of the formula (II) ##STR2## in which X is the equivalent of an anion of an organic or inorganic acid having a pKa value of less than 7,b) reacting the diazonium salt of the formula (II) with a methacrylic acid derivative of the formula (III) ##STR3## in which R is as defined above in the presence of a palladium catalyst, if desired in the presence of a base and/or a solvent, to give the compounds of the formulae (IV) and (V) in which R is as defined above, ##STR4## and c) hydrogenating the resulting compounds of the formulae (IV) and (V) in the presence of a palladium catalyst with hydrogen.

Abstract: .alpha.-(trifluoromethyl)arylacetic acid for use as raw materials for medicines, agricultural chemicals, liquid crystals etc. or reagents for determining an optical purity is readily obtained through very simple reaction steps, i.e. by reacting a perfluoro(2-methyl-1,2-epoxypropyl)ether compound obtainable by ozone, oxidation of a heptafluoroisobutenyl ether compound with an aromatic compound ArH to afford an .alpha.,.alpha.-bis(trifluoromethyl)arylacetic acid ester, followed by decarboxylation and hydrolysis of the resulting ester compound.

Abstract: (S)-ibuprofen may be separated from a mixture of (S)-ibuprofen and (R)-ibuprofen in high yield and enantiomeric purity in a single resolution step using an N-alkyl-D-glucamine as the resolving agent.

Abstract: The present invention provides a novel 2-aralkyl-3-chloropropionic acid and a process for the preparation thereof. A novel 2-aralkyl-3-chloropropionic acid is represented by the general formula (1): ##STR1## and can be prepared by asymmetrically hydrogenating a (Z)-2-aralkylidene-3-chloropropionic acid represented by the general formula (II): ##STR2## with a complex of a bidentate phosphine with ruthenium as a catalyst in the presence of a tertiary amine.

Abstract: The present invention concerns a process for the production of compositions of 2-arylpropionic acid derivatives with improved tablettability which contain per se known adjuvant and/or carrier materials, whereby the arylpropionic acid is mixed with a calcium compound and, after addition of the remaining adjuvant and/or carrier materials, is pressed to tablets, as well as pharmaceutical compositions produced therewith.

Abstract: A process for the production of an optically active carboxylic acid (I), which comprises subjecting an olefinic carboxylic acid (II) to asymmetric hydrogenation using a complex as a catalyst consisting of an optically active phosphine (III) and a ruthenium compound.Complex of ##STR1## with a ruthenium compound ##STR2## According to the process of the present invention, optically active carboxylic acids can be produced with high yield.

Abstract: A description is given of carrier-bound compounds of the formula I ##STR1## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 independently of one another are hydrogen, halogen, nitro, cyano, CF.sub.3, C.sub.1 -C.sub.15 alkyl, C.sub.5 -C.sub.12 cycloalkyl, C.sub.2 -C.sub.15 alkenyl, C.sub.1 -C.sub.12 haloalkyl, C.sub.1 -C.sub.12 alkoxy, C.sub.1 -C.sub.12 alkylthio, C.sub.6 -C.sub.10 aryl, C.sub.6 -C.sub.10 aryloxy, C.sub.7 -C.sub.12 arylalkyl, --CO.sub.2 R.sub.6, --COR.sub.6 or ##STR2## in which at least one of the radicals R.sub.1 to R.sub.5 is hydrogen, halogen or C.sub.1 -C.sub.15 alkyl, and, in addition, the radicals R.sub.1 and R.sub.2, R.sub.2 and R.sub.3, R.sub.3 and R.sub.4 or R.sub.4 and R.sub.5 together with the carbon atoms to which they are attached form a benzo or cyclohexenyl ring,R.sub.6 is C.sub.1 -C.sub.20 alkyl, C.sub.2 -C.sub.20 alkyl which is interrupted by oxygen, sulfur or >N--R.sub.9 ; or is C.sub.7 -C.sub.12 arylalkyl,R.sub.7 and R.sub.

Abstract: A novel neomorphic form of ibuprofen, processes for preparing the ibuprofen, and method for administering the ibuprofen are provided. The neomorphic form is characterized by having a distinctively less bitter taste and causes less burning sensation upon swallowing. The neomorphic form of ibuprofen contains an amorphous ibuprofen. Tests indicate that the neomorphic form is less irritating to the gastrointestinal tract of animals upon administration.

Abstract: A process for the preparation of salts of 2-(4-isobutylphenyl)propionic acid with basic aminoacids, in particular L-arginine and L-lysine, is described.

Abstract: There are described novel alkaline earth metal salts, transition metal salts and transition metal complexes of compounds of the formula I ##STR1## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are, independently of one another, hydrogen, halogen, nitro, cyano, CF.sub.3, C.sub.1 -C.sub.15 alkyl, C.sub.5 -C.sub.12 cycloalkyl, C.sub.2 -C.sub.15 alkenyl, C.sub.1 -C.sub.12 haloalkyl, C.sub.1 -C.sub.12 alkoxy, C.sub.1 -C.sub.12 alkylthio, C.sub.6 -C.sub.10 aryl which is unsubstituted or substituted by C.sub.1 -C.sub.4 alkyl; C.sub.6 -C.sub.10 aryloxy which is unsubstituted or substituted by C.sub.1 -C.sub.4 alkyl; C.sub.7 -C.sub.12 arylalkyl which is unsubstituted or substituted on the aryl radical by from 1 to 3 C.sub.1 -C.sub.4 alkyl groups; --CO.sub.2 R.sub.6, --COR.sub.6 or ##STR2## where at least one of the radicals R.sub.1 to R.sub.5 is hydrogen, halogen or C.sub.1 -C.sub.15 alkyl, in addition the radicals R.sub.1 and R.sub.2, R2 and R.sub.3, R.sub.3 and R.sub.4 or R.sub.4 and R.sub.

Abstract: The subject matter of the invention is a process for the preparation of carboxylic acids and derivatives of them of the general formula ##STR1## wherein R means hydrogen, or a C.sub.1-4 alkyl or a (C.sub.1-5 alkoxy)carbonyl group,R.sub.1 is as defined in claim 1,R.sub.7 stands for hydrogen or a C.sub.1-7 alkyl group andR.sub.8 means hydrogen or a carboxyl group.

Abstract: Disclosed herein is a process of making chiral 2-aryl-1,4-butanediamine derivatives useful as neurokinin-A antagonists of Formula 7 ##STR1##