Abstract: A novel 3-aryl-2-hydroxypropionic acid derivative, a process and intermediate for its manufacture, pharmaceutical preparations containing it and the use of the compound in clinical conditions associated with insulin resistance.

Abstract: The present invention relates to an improved process for the preparation of trifluoromethanesulfonic ester of ethyl (R)-2-hydroxy-4-phenylbutyrate, referred to here as triflate in structural Formula I, and to the use of this compound as intermediate for the preparation of ACE (Angiotensin Converting Enzyme) inhibitor, benazepril.

Abstract: The present invention provides new compounds that can be used as antioxidants for either molecules that do not conation ester groups or esters of alcohols that contain two or more ester groups per molecule wherein at least two of the ester groups are on adjacent carbons in the alcohol moiety. Copper ions can enhance the antioxidization activity of the new compounds. Compositions containing one of the new compound and methods of using the new compounds are disclosed.

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-&agr;-aspartyl]-L-phenylalanine 1-methyl ester, which is a sweetener with high sweetening potency.

Abstract: The present invention relates to certain tri-substituted phenyl derivatives and analogues of formula (I), to a process for preparing such compounds, having the utility in clinical conditions associated with insulin resistance, to methods for their therapeutic use and to pharmaceutical compositions containing them.

Abstract: Methyl (R)-2-(R1OSO2)-2-(2-chlorophenyl)acetates useful as intermediates in the preparation of methyl (S)-2(2-chlorophenyl)-2-(4,5,6,7-tetrahydrothieno[3,2-c]-5-pyridyl)acetate.

Abstract: The invention relates to new compounds of general formula I 1

Abstract: The present invention provides new synthetic methods and compositions. In particular, new methods of preparing intermediates useful in the synthesis of neuraminidase inhibitors and compositions useful as intermediates that are themselves useful in the synthesis of neuraminidase inhibitors are provided.

Abstract: The present invention provides a linker binding carrier for organic synthesis represented by the formula: —Z—W—(SO2X)m wherein  is a carrier, X is a leaving group, Y is a bond or spacer, Z is a bivalent group, when Z is a bivalent electron attractive group, W is an aromatic ring which may be substituted and when Z is a bivalent non-electron attractive group, W is an aromatic ring which is substituted by an electron attractive group and may be further substituted and m is 1 or 2, or a salt thereof, which is useful for synthesizing a novel organic compound.

Abstract: In accordance with the present invention, there are provided normal modified forms of nonsteroidal anti-inflammatory drugs. Modified NSAIDs according to the invention provide a new class of anti-inflammatory agent which provide the therapeutic benefits of NSAIDs while causing a much lower incidence of side-effects then typically observed with such agents.

Abstract: Novel tricyclic compounds of formula I as defined in the specification, a process for their preparation and their use for the preparation of optically active or racemic colchicine and thiocolchicine derivatives.

Abstract: Compounds of Formula 1 and of Formula 2 where the symbols have the meaning defined in the specification, have retinoid, retinoid antagonist or retinoid negative hormone like biological activity.

Abstract: Optically active 2-aralkyl-3-sulfonyloxy-1-propanol and 2-aralkyl-3-sulfonyloxypropionic acid are provided by using an optically active 2-aralkyl-3-acyloxy-1-propanol as a starting material. Furthermore, an optically active 2-aralkyl-3-thiopropionic acid, which is an important intermediate for synthesis of enkephalinase inhibitors, is provided. According to the present invention, industrially useful optically active sulfonic acid ester derivatives can be provided.

Abstract: There are disclosed novel sulfamate compounds containing N-substituted carbomoyl group including their racemates and (R)- and (S)-optical isomers represented by Formulas I, II and III, pharmaceutically useful for the prophylaxis and treatment of the disorders of the central nervous system, especially for nervous myalgia, epilepsy and minimal brain dysfunction: ##STR1## (III).

Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is C.sub.3 -C.sub.8 cycloalkyl, halo-C.sub.3 -C.sub.8 cycloalkyl, C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.6 alkyl, halo-C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.6 alkyl, --Si(R.sub.3).sub.3, --S--R.sub.4, --SO.sub.2 --R.sub.6 or --CO--R.sub.9 ;R.sub.2 is halogen, C.sub.1 -C.sub.4 alkyl or CF.sub.3, the substituents R.sub.2 being identical or different when n is 2;R.sub.3 each independently of the others is C.sub.1 -C.sub.6 alkyl, halo-C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy or phenyl;R.sub.4 is aryl or heteroaryl each of which is unsubstituted or substituted;R.sub.6 is unsubstituted or substituted C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.1 -C.sub.20 -alkoxy, C.sub.2 -C.sub.6 alkenyloxy, C.sub.2 -C.sub.6 alkynyloxy, C.sub.1 -C.sub.4 alkylthio, aryl, aryloxy or arylthio, or is optionally substituted amino;R.sub.9 is hydroxy, unsubstituted or substituted C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.6 alkenyl, C.

Abstract: A compound of the general formula(M.sup.1).sub.n -Q-(M.sup.2).sub.1-n -L-A Iwherein: n is 0 or 1;M.sup.1 is an amino group;Q is an aromatic heterocyclic group containing a basic nitrogen atom;M.sup.2 is an imino group;L is a template group; andA is an acidic group, or an ester or amide derivative thereof, or a sulphonamide group;and pharmaceutically acceptable salts and pro-drugs thereof, for use in the treatment of a disease in which platelet aggregation mediated by the binding of adhesion molecules to GPIIb-IIIa is involved and the optically active compound (-)-(3R)-3-methyl-4-{4-?4-(4-pyridyl)-piperazin-1-yl!phenoxy}butyric acid is also disclosed.

Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.

Abstract: Nitrogen mustard pro-drugs of the formula ##STR1## are disclosed where R is the residue of an .alpha.-amino acid RNH.sub.2 and M is a disubstituted amino "mustard" group, useful in antibody directed enzyme pro-drug therapy in the treatment of cancer.

Abstract: A compound of the formula ##STR1## wherein R.sub.1 is a straight or branched alkyl group having from 1 to 6 carbon atoms, phenyl, or cycloalkyl having from 3 to 6 carbon atoms; R.sub.2 is hydrogen or methyl; and R.sub.3 is hydrogen, methyl or carboxyl; which is useful in the treatment of seizure disorders. Processes are disclosed for the preparation of the compound. Intermediates prepared during the synthesis of the compound are also disclosed.

Abstract: Novel tricyclic compounds of formula I as defined in the specification, a process for their preparation and their use for the preparation of optically active or racemic colchicine and thiocolchicine derivatives.

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 synthesizing enantiomerically pure chiral secondary alcohol compounds linked to a heterocyclic core moiety, using a natural chiral molecule starting material. The inventive process is particularly useful for bulk manufacturing of chiral secondary alcohol compounds.

Abstract: A compound of the formula ##STR1## wherein R.sub.1 is a straight or branched alkyl group having from 1 to 6 carbon atoms, phenyl, or cycloalkyl having from 3 to 6 carbon atoms; R.sub.2 is hydrogen or methyl; and R.sub.3 is hydrogen, methyl or carboxyl; which is useful in the treatment of seizure disorders. Processes are disclosed for the preparation of the compound. Intermediates prepared during the synthesis of the compound are also disclosed.

Abstract: A process for the preparation of trialkyl ester derivatives of the general formula: ##STR1## wherein X is chlorine, bromine, iodine, tosyloxy or mesyloxy and R is a C.sub.1 -C.sub.6 -alkyl group. According to this process, a trialkyl methanetricarboxylate of the general formula: ##STR2## wherein R has the meaning given above, is converted to the end product of formula I with a disubstituted ethane of the general formula:X--CH.sub.2 --CH.sub.2 --X IIIwherein the two substituents X are identical or different and have the meaning given above, in the presence of an alkaline earth metal carbonate or alkali metal carbonate.

Abstract: A process for preparing fluorocarbon fluoroalkanesulfonates comprises (a) forming a mixture comprising at least one fluoroalkanesulfonyl halide, e.g., perfluoromethanesulfonyl fluoride, at least one fluorocarbon-substituted carbinol, e.g., 1,1-dihydroperfluorobutoxyethoxyethanol, and at least one base, e.g., triethyl amine; and (b) allowing the mixture to react in the absence of solvent at a temperature below ambient. The process is volume-efficient and provides high yields of fluorocarbon fluoroalkanesulfonates useful as intermediates in, e.g., drug synthesis.

Abstract: A process is described for the preparation of (+)-2-(3,4-dichlorophenyl)-4-hydroxybutylamine (I) by reaction of 3,4-dichlorophenylacetonitrile (II) with an alkali metal halogenoacetate, treatment of the 3-cyano-3-(3,4-dichlorophenyl)propionic acid (III) with D-(-)-N-methylglucamine, with second-order asymmetric conversion, hydrolysis of the D-(-)-N-methylglucamine salt of (-)-3-cyano-3-(3,4-dichlorophenyl)propionic acid and enantioconservative reduction of the resulting levorotatory cyanoacid with a borane.

Abstract: .beta.-Carboxy sulfonates of the formula ##STR1## wherein R.sub.1 is aryl, R.sub.3 and R.sub.4 are hydrogen or alkyl, Y is -O-, -S-, or -NR.sub.2 -, and R.sub.5 is alkyl or aryl are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT) and are thus useful for treating hypercholesterolemia and atherosclerosis.

Abstract: Compounds are described which are S-(.omega.-hydroxyalkyl) esters of thioacrylic and thiomethacrylic acids. The compounds have the formula: ##STR1## wherein: R is hydrogen or methyl; andn is 1, 2 or 3.These compounds can be used as conditioners to enhance the wettability of dentinal surfaces, can be employed as chemical tracers to characterize the wetting of dentinal surfaces, and can be copolymerized in situ to form potential dentinal bonding systems. The compounds can also be homopolymerized and copolymerized to form other useful products.

Abstract: A process is disclosed for the separation of an enantiomerically enriched 1-tosyloxy-2-acyloxy-3-butene and an enantiomerically enriched 1-tosyloxy-2-hydroxy-3-butene from a first mixture containing both compounds. The process includes the steps of:(a) forming a solution of the mixture in an organic solvent;(b) bringing the solution formed in (a) to a temperature wherein most of the enantiomerically enriched 1-tosyloxy-2-hydroxy-3-butene precipates, leaving in solution most of the enantiomerically enriched 1-tosyloxy-2-acyloxy-3-butene; and(c) separating the precipitate formed in (b) from the solution.

Abstract: The invention provides compounds of formula (I): ##STR1## or a physiologically acceptable salt or solvate thereof wherein R.sup.1 represents a halogen or hydrogen atom or a C.sub.1-6 alkyl or C.sub.1-6 alkoxy group;R.sup.2 represents a phenyl group optionally substituted by one or two substituents;R.sup.3 represents the group ##STR2## R.sup.4 and R.sup.5, which may be the same or different, each independently represent a hydrogen atom or a halogen atom, or a group selected from hydroxy, C.sub.1-6 alkoxy or C.sub.1-6 alkyl.The compounds may be used in the treatment or prophylaxis of depression and other CNS disorders.

Abstract: The present invention relates to a synthetic method of optically active starting materials for various medicaments, which are represented by Formula (I): ##STR1## wherein R.sup.1 is hydrogen or hydroxy protecting group; * is an asymmetric carbon; R.sup.2 ' is hydrogen or an optionally substituted lower alkyl; and Q is --CH.dbd.P(Ph).sub.3, --CH.sub.2 P(O)(OMe).sub.2, or --CH.sub.2 S(O)Me, in high optical purity on a large scale.In more detail, the present invention provides intermediates and a method for the production thereof for synthesizing optically active compounds which are able to inhibit activities of HMG-CoA reductase and are, therefore, useful for inhibition of cholesterol biosynthesis.

Abstract: Novel monocyclic terpene derivative of the formula: ##STR1## wherein R is hydrogen atom, trimethylsilyl group or 1-ethoxyethyl group, and novel intermediates therefor. The terpene derivative (I) is a useful intermediate for preparing Sarcophytol A having an anti-carcinogenesis promoter activity and an antitumor activity.

Abstract: Chiral epoxybutyrates are prepared in high yield from novel dihydro-3R-substituted sulfonyloxy-4R-hydroxy-2-(3H)furanones via based catalyzed alcoholysis. The product chiral epoxy butyrates are useful intermediates for the synthesis of 1-carba-1-dethia cephem antibiotics.

Abstract: Novel 2,2-dimethyl-cyclopropane carboxylic acid derivatives of the formula ##STR1## wherein X.sub.1 and X.sub.2 are individually halogen, R.sub.1 is selected from the group consisting of halogen, alkyl of 1 to 8 carbon atoms, optionally substituted aryl of 6 to 14 carbon atoms, perfluoroalkyl of 1 to 8 carbon atoms, --CN and ##STR2## R' is alkyl of 1 to 8 carbon atoms, Y is selected from the group consisting of --SO.sub.2 Alk.sub.1, --SO.sub.2 Ar, ##STR3## Alk.sub.1 is optionally unsaturated alkyl of 1 to 8 carbon atoms optionally substituted with at least one halogen, Ar is aryl of 6 to 14 carbon atoms optionally substituted with at least one halogen Alk.sub.2 and Alk.sub.3 and Alk.sub.2 ' and Alk.sub.

Abstract: The present invention provides an optically active 2-methylenepentane derivative represented by the general formula ##STR1## (wherein R.sup.1 is a protective group for hydroxyl, R.sup.3 is a protective group for hydroxyl, X is a halogen atom or R.sup.4 SO.sub.3 group (wherein R.sup.4 is an alkyl or an aryl), and the symbol * represents an asymmetric carbon atom).

Abstract: Optically active naphthyl alpha-substituted alkyl ketones, are a class of ketones useful as intermediates in the production of optically active alpha-naphthylalkanoic acids which exhibit anti-inflammatory, analgesic and anti-pyretic activity.

Abstract: Novel aryl ethers, containing both a carboxylic acid and a sulfonic acid functionality; and a process for making them are described. These difunctional aryl compounds comprise:i) a carboxylic acid group or its derivative,ii) a first aromatic group bonded to the carboxylic acid or its derivative,iii) a second aromatic group linked to the first aromatic group by a non-electron-withdrawing moiety,iv) a third aromatic group linked to the second aromatic group by a non-electron-withdrawing moiety, andv) a sulfonyl group or its derivative bonded to the third aromatic group.

Abstract: A process is disclosed for the preparation of aliphatic toluenesulfonates. The process comprises reacting a solution of an aliphatic alcohol and an alkali metal hydroxide in a solution of an aprotic solvent with toluenesulfonyl chloride for from about 1 to about 12 hours and forming said aliphatic toluenesulfonate. These compounds are useful intermediates in the preparation of complex organic molecules.

Abstract: (-)-Swainsonine is prepared by the steps of first reacting a compound having the formula: ##STR1## wherein each R.sub.2 is lower alkyl, with (4-carbalkoxybutyl) triphenylphosphonium bromide in a strong base to obtain an alcohol having the formula: ##STR2## wherein R.sub.2 is as defined above and R is C.sub.1 -C.sub.8 alkyl; the alcohol is then reacted with methanesulfonyl chloride or p-toluenesulfonyl chloride or benzenesulfonyl chloride in the presence of a tertiary amine to obtain the corresponding sulfonate. Heating the sulfonate with an azide in an organic solvent yields an imine having the formula: ##STR3## wherein R.sub.2 and R are ad defined above. Treating the imine with an inorganic base, in aqueous alcohol provides upon acidification, the corresponding acid. Heating the acid at reflux temperature in organic solvent, yields an enamide having the formula: ##STR4## wherein R.sub.2 is as defined above.

Abstract: Conjugated diene compounds of the general formula: ##STR1## which are industrially advantageous intermediates for preparing sarcophytol A useful as an anticarcinogenic promotor or antitumor agent are provided.

Abstract: A UCN-1028D derivative represented by the formula: ##STR1## has protein kinase C inhibitory activity and is expected to be used as an active ingredient in anti-tumor agents, etc.

Abstract: A process is disclosed for the isolation of an enantiomerically enriched alcohol from a first mixture of an enantiomerically enriched 1-arylsulfonate-2 -hydroxy-3-butene and an enantiomerically enriched 1 -arylsulfonate- 2-acyloxy-3-butene. The process includes the steps of:(a) contacting the mixture with a reagent capable of reacting with said 1-arylsulfonate-2-hydroxy-3-butene to remove the arylsulfonate group and produce a mixture of dihydroxybutene monoesters thereby forming a second mixture containing said dihydroxybutene monoesters and unreacted enantiomerically enriched 1-arylsulfonate-2-acyloxy-3-butene(b) contacting the second mixture with reagents capable of hydrolyzing all of the acyl groups in said mixture to hydroxy groups so as to produce a third mixture comprising 1,2-dihydroxy-3-butenes and enantiomerically enriched 1-arylsulfonate-2-hydroxy-3 -butene;(c) washing said third mixture with water so as to remove said 1,2-dihydroxy-3-butenes.

Abstract: A process is disclosed for the isolation of an enantiomerically enriched alcohol from a first mixture of an enantiomerically enriched alcohol and an enantiomerically enriched ester. The process includes the steps of:(a) contacting the mixture with a reagent capable of reacting with the hydroxy function of the alcohol, without the loss of optical purity, so as to produce a second mixture containing a base stable derivative of the enantiomerically enriched alcohol and the unreacted ester;(b) contacting the second mixture with a base capable of reacting with the ester so as to produce a third mixture containing a compound more volatile than the base stable derivative of the alcohol;(c) removing the volatile compound from the third mixture; and(d) converting the base stable derivative of the alcohol back to the enantiomerically enriched alcohol, without the loss of optical purity.

Abstract: Isocyanatoalkyl sulphonates of the general formula ##STR1## wherein the substituent meanings are as given in the description are obtained by reacting the corresponding isocyanatoalkyl halides with sulphonic acid esters of the formula ##STR2## wherein R.sup.3 has the meanings given in the description. They are used as cross-linking agents in polyamines.

Abstract: Chiral epoxybutyrates are prepared in high yield from novel dihydro-3R-substituted sulfonyloxy-4R-hydroxy-2-(3H)furanones via based catalyzed alcoholysis. The product chiral epoxy butyrates are useful intermediates for the synthesis of 1-carba-1-dethia cephem antibiotics.

Abstract: The invention relates to novel sulfonic acid esters of formula I ##STR1## wherein R.sup.1 is C.sub.5 -C.sub.6 cycloalkyl which is unsubstituted or substituted by C.sub.1 -C.sub.7 alkyl, unsubstituted or substituted phenyl, R.sup.2 is C.sub.1 -C.sub.7 alkyl, R.sup.3 is phenyl which is substituted by halogen or nitro, and the asterisk denotes a carbon atom that is either present in the preponderant number of molecules in the S configuration or in the preponderant number of molecules in the R configuration.These compounds can be prepared by enantio-selective reduction of 4-R.sup.1 -substituted .alpha.-oxobutyric acid compounds and subsequent conversion of the resultant .alpha.-hydroxy group into the --OSO.sub.2 --R.sup.3 group. The compounds of formula I are suitable intermediates for the preparation of ACE inhibitors or precursors thereof.

Abstract: Hydroxyalkylating agents of formula: ##STR1## in which R denotes alkyl, n is 2 or 3, R.sub.1 denotes hydrogen or alkyl and R.sub.2 denotes alkyl an unsubstituted or substituted phenyl or ##STR2## are useful inter alia for the preparation of 1-(hydroxyalkyl)imidazoles. They are made by reaction of a sulphonic acid or dimethyl sulphate with a corresponding decarboxylate ester.

Abstract: A compound of a 3,5,6-trihydroxyhexanoic acid derivative of the formula: ##STR1## wherein P.sup.1 and P.sup.2 are independently hydrogen atoms or hydroxy-protecting groups, or together form a ring, and R is an alkyl group is effectively prepared by a process comprising steps of:reacting a butyronitrile derivative of the formula: ##STR2## wherein P.sup.1 and P.sup.2 are the same as defined above with an .alpha.-haloacetate of the formula:X--CH.sub.2 --COOR (III)wherein X is a halogen atom, and R is the same as defined above in the presence of a metallic catalyst selected from the group consisting zinc and zinc-copper to form a keto acid derivative of the formula: ##STR3## wherein P.sup.1, P.sup.2 and R are the same as defined above, and then reducing the obtained keto-acid derivative of the formula (IV).

Abstract: Optically active periplanone-B is manufactured through oxidizing (1RS, 4S, 5E)-isopropyl-7-methylene-5-cyclodecene-1-ol. The oxidized product is regioselectively enolized and then sulfenylated. The sulfenylated product is oxidized and then subjected to decomposition of the sulfoxide. The decomposed product is epoxidated, and the epoxidated product is converted into an enolate which is then oxidized. The oxidized product is oxidized and then regio- and stereoselectively epoxidated to obtain optically active periplanone-B.

Abstract: Carbacyclin derivatives of Formula I ##STR1## wherein R.sub.1 is hydrogen or OR.sub.2, wherein R.sub.2 is hydrogen, alkyl, cycloalkyl, aryl, ##STR2## or a heterocyclic residue; or R.sub.1 is NHR.sub.3 wherein R.sub.3 is an acid residue (acyl) or R.sub.2,n is 2, 3, 4, or 5,X is hydrogen or fluorine,A is --CH.sub.2 --CH.sub.2 --, trans--CH.dbd.CH--, or --C.tbd.C--,W is a free or functionally modified hydroxymethylene group or a free or functionally modified ##STR3## wherein the OH-group can be in the .alpha.- or .beta.-position, D is ##STR4## a straight-chain, saturated aliphatic group of 1-10 carbon atoms, a branched, saturated or a straight-chain or branched, unsaturated aliphatic group of 2-10 carbon atoms, all of which can optionally be substituted by fluorine atoms,m is 1, 2, or 3,E is a direct bond, --C.tbd.C--, or --CR.sub.6 .dbd.CR.sub.7 -- wherein R.sub.6 and R.sub.7 are different from each other and are hydrogen or alkyl or 1-5 carbon atoms, or are hydrogen or halogen,R.sub.