Abstract: The invention relates to a process for the production of prostaglandin precursors of formula I ##STR1## as well as their enantiomers in which X is A--W or W--A,A is a --C.tbd.C-- group,W is a hydroxymethylene group, in which the OH group can be functionally modified by etherification or esterification,D is a straight-chain or branched-chain alkylene group with 2-5 C atoms each or a ##STR2## group, n i s 1 to 3,E is a --C.tbd.C-- group or a --CR.sub.3 .dbd.CR.sub.4 group with R.sub.3 and R.sub.4 each meaning a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group,R.sub.1 is a hydrogen atom or a hydroxy group, which can be functionally modified as in W,R.sub.2 is a straight-chain or branched-chain alkyl group with 1-7 C atoms, characterized in that vinyl bromides of formula II ##STR3## in which Z means the group ##STR4## and R.sub.1, W, D, E and R.sub.2 have the above-indicated meanings and hydroxy groups unprotected in R.sub.1 and W or represented by an optionally substituted benzoyl radical, a C.sub.1 -C.sub.

Abstract: This invention relates to compounds of structural formula (I): ##STR1## which are squalene synthase inhibitors and thus useful as cholesterol lowering agents and antifungal agents. These compounds are also inhibitors of farnesyl protein transferase and farnesylation of the oncogene protein Ras and thus useful in treating cancer.

Abstract: New cholesterol lowering compounds are formed from the photochemical treatment of zaragozic acid A.

Abstract: A process for the preparation of a compound of Formula (1): ##STR1## wherein: W.sup.1 is aryl;X.sup.1 and X.sup.2 are each independently selected from --H, --CN, halogen, alkyl, aryl and --COOH;Y is --H;Z is --OH; orY and Z together form a group of Formula (2): ##STR2## wherein: W.sup.2 is aryl;which comprises reacting a compound of Formula (3): ##STR3## wherein: X.sup.1, X.sup.2, Y and Z are as hereinbefore defined with a compound of Formula (4): ##STR4## wherein the substituents are as defined in the specification.

Abstract: A process is disclosed for treating polyamide fiber containing materials which process comprises applying a benzofuran-2-one compound to the material in order to enhance its moulding stability. In addition, compositions containing a fluorescent whitening agent and a benzofuran-2-one, and optionally one or more dyes, are disclosed.

Abstract: A single step process for converting aldaric acid salts to activated aldarates utilizing a lower alkanol as both solvent and esterifying agent is described. The activated aldarates are particularly useful as monomers for polymerizations with primary diamines in which the nitrogen atoms are bound to aliphatic carbon atoms to form poly(aldaramides).

Abstract: A benzofuranone of the Formula (1): ##STR1## wherein: R.sup.1 and R.sup.2 are each independently --H or optionally substituted C.sub.1-20 -alkyl;R.sup.3 and R.sup.4 are each independently --H or optionally substituted C.sub.1-6 -alkyl;R.sup.5 is selected from --H, --CN, --COOR.sup.10 and --COR.sup.10, in which R.sup.10 is --H or C.sub.1-6 -alkyl;R.sup.6, R.sup.7, R.sup.8 and R.sup.9 are each independently selected from --H, --NR.sup.1 R.sup.2, --NO.sub.2, halogen, optionally substituted C.sub.1-6 -alkyl and optionally substituted C.sub.1-6 -alkoxy.

Abstract: Compounds which are benzofuran-2-ones having two organothiomethyl substituents directly attached to the benzo ring are suitable for stabilizing organic materials against thermal, oxidative or light-induced degradation.

Abstract: The present invention provides a method of preparing .alpha.,.beta.-unsaturated ketolactones which are useful for production of prostaglandins having one or more halogen substituent(s) at the 16 or 17 portion in high yield, in which, a dimethyl (2-oxoalkyl) phosphonate having one or more halogen substituents, a starting material, is reacted with a bicyclolactone aldehyde under the presence of an alkali metal hydride and a zinc compound.

Abstract: Compounds of formula I ##STR1## wherein R.sub.1 is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.5 -C.sub.8 cycloalkyl or C.sub.7 -C.sub.9 phenylalkyl, A.sub.1 and A.sub.4 are phenyl, ##STR2## or phenyl which is substituted by 1 to 3 radicals R.sub.3, which radicals R.sub.3 are each independently of one another selected from the group consisting of C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.18 alkoxy, C.sub.3 -C.sub.4 alkenyloxy, C.sub.7 -C.sub.9 phenylalkoxy, C.sub.5 -C.sub.8 cycloalkoxy, C.sub.1 -C.sub.18 alkanoyloxy, C.sub.3 -C.sub.18 alkenoyloxy, benzoyloxy, phenoxy and hydroxy, m is 1 or 2, A.sub.2 and A.sub.3, together with the linking carbon atom, form a C.sub.5 -C.sub.7 cycloalkylidene ring which is unsubstituted or substituted by 1 to 3 C.sub.1 -C.sub.4 alkyl groups, are very suitable for stabilising organic materials against thermal, oxidative or light-induced degradation.

Abstract: Variously substituted 4-(biphen-2-ylmethylcarbamoyl)-3-hydroxybutyric acids and esters, also named as N-(biphen-2-yl)-3-hydroxyglutaramic acid derivatives, are blood cholesterol lowering agents and so are useful in the prevention and treatment of cardiovascular diseases such as atherosclerosis.

Abstract: A Derivative of 5-hetero-6-oxo-PGE A derivative of 5-hetero-6-oxo-PGE of the formula: ##STR1## wherein R.sup.1 is (1) a group of the formula: COOR11(2) hydroxymethylcarbonyl,(3) hydroxymethyl or(4) a group of the formula:CO--AAwherein AA is an amino acid-residue,Z is oxygen, sulfur or a group of the formula: NR21 wherein R21 is hydrogen or alkyl of C1--4;R2 is a single-bond or alkylene of C1--4;R3 isi) alkyl of C1-7,ii) cycloalkyl of C4-7 or cycloalkyl of C4-7 substituted by alkyl of C1-7,iii) phenyl, phenoxy, phenyl or phenoxy substituted by one group selected from alkyl of C1-4, halogen and trihalomethyl, is single-bond or a double bond.Possess PG-like activity, especially cytoprotection, and therefore are useful for treatment for and/or prevention of cytodamage.

Abstract: 2-Propyl-2-pentanoic acid (valproic acid) esters and (E)-2-propyl-2-pentenoic acid [(E)-2-valproenoic acid] esters surprisingly proved to have valuable properties, in that they show anticonvulsive and antiepileptic activities comparable with those of valproic acid, as well as an improved bioavailability and a markedly reduced toxicity.

Abstract: 13-alkyl-11.beta.-phenyl-gonanes of general formula I ##STR1## wherein A and B together stand for an oxygen atom, a CH.sub.2 group or a second bond between carbon atoms 9 and 10,X is an oxygen atom or the hydroxyimino grouping N.about.OH,R.sub.1 is a straight-chained or branched, saturated or unsaturated alkyl radical with up to 8 carbon atoms, which contains the grouping ##STR2## with X as described above, R.sub.2 is a methyl or ethyl radical in the .alpha. or .beta. position,R.sub.9, R.sub.10, R.sub.11 and R.sub.12 each stand for a hydrogen atom, a hydroxy, alkyl, alkoxy or acyloxy group with 1 to 4 carbon atoms respectively or a halogen atom and R.sub.3 and R.sub.4 have a variety of meanings, have antigestagenic and antiglucocorticoid effects.

Abstract: Diphenyl ether derivatives of formula II ##STR1## wherein R.sub.1 represents a hydrogen or halogen atom or an alkyl or haloalkyl group, R.sub.2 and R.sub.3, which may be the same or different, each independently represents a hydrogen or halogen atom, or an alkyl, haloalkyl, nitro or cyano group, R.sub.4 represents an alkyl group and X represents an oxygen or sulphur atom, useful as intermediates in the preparation of diphenyl ether herbicides, are prepared by treating a compound of formula III ##STR2## where R.sub.1, R.sub.2, R.sub.3 and X are as defined above and R.sub.6 is a hydrogen atom or an alkyl group, with an alkali under hydrolyzing conditions.

Abstract: Azulene derivatives of the following formula ##STR1## wherein R.sup.1 stands for an alkyl group of 1 to 3 carbon atoms, R.sup.2 stands for an alkyl group of 1 to 3 carbon atoms, and R.sup.3 is at the 5- or 6-position and stands for an alkyl group of 1 to 6 carbon atoms, an aryl group of 6 to 9 carbon atoms or an aralkyl group of 7 to 10 carbon atoms; have antihyperlipidemic activity. Many of the compounds are also novel per se.

Abstract: A process for the preparation of oxophthalazinyl acetic acids having benzothiazole or other heterocyclic side chains comprising reacting an oxophthalizinyl acetic acid ester with an aniline derivative is disclosed. Also disclosed are processes for the preparation of such oxopthalizinyl esters.

Abstract: A compound of the formula ##STR1## in its d, 1 or d1 form and mixtures thereof and their preparation and their use in the synthesis of pyrethrinoids.

Abstract: Oxophthalazinyl acetic acids having aldose reductase inhibitory properties of the formula ##STR1## wherein Z is hydrogen or methyl, U is S, CH.sub.2 or a covalent bond, and R.sup.1, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are as herein defined, are prepared by reacting an intermediate oxophthalazinyl acetic acid ester having a cyano or alkylamido group with an aniline derivative of the formula ##STR2## Processes for the preparation of the intermediate oxophthalazinyl acetic esters are disclosed.

Abstract: The invention relates to new 2-(2,3-dihydro-2-oxo-3-benzofuranyl)acetic acid compounds of general formula I: ##STR1## in which: R.sub.1 denotes a hydrogen atom, a linear or branched alkyl radical having 1 to 4 carbon atoms or a phenyl radical optionally substituted with a halogen atom or with an alkoxy radical containing 1 to 4 carbon atoms or an alkyl radical having 1 to 4 carbon atoms,R.sub.2 denotes a hydrogen or halogen atom, a hydroxyl radical, an alkyl radical having 1 to 4 carbon atoms or an alkoxy radical containing 1 to 4 carbon atoms,R denotes a hydroxyl radical, a linear or branched alkoxy radical having 1 to 4 carbon atoms, a benzyloxy radical or a radical of general formula A: ##STR2## in which: X and Y, which may be identical or different, each denote a linear or branched alkyl radical containing 1 to 5 carbon atoms, a radical of general formula A.sub.

Abstract: Racemic carboxylic acids are resolved into their enantiomers using optically active enantiomers of four lactones as resolving agents. The four lactones are 2,3-isopropylidene-ribonic acid-1,4-lactone, 1,2-isopropylidene-glucofuranurono-3,6-lactone, 2-hydroxy-3,3-dimethyl-1,4-butyrolactone and 3,4-isopropylidene-arabino-1,5-lactone. Novel diastereoisomeric esters of the acids with the lactones are disclosed.

Abstract: Cromoglycic acid derivatives of the general formula ##STR1## wherein R.sup.1 is an .alpha.-, .beta.- or .gamma.-amino acid residue (for ester bonding) whose amino group may optionally be substituted by at least one lower alkyl group, and R.sup.2 and R.sup.3 each independently is a lower alkyloxy-substituted or an unsubstituted lower alkyl group, an 1-alkanoyloxyalkyl group, an 1-alkoxycarbonyloxyalkyl group, a phthalidyl group or a 5-methyl-1,3-dioxol-2-on-4-ylmethyl group; nontoxic salts thereof; and pharmaceutical compositions containing such compounds. Since the compounds have antiallergic activity and are readily absorbable into the blood stream, they are useful as oral antiallergic agents.

Abstract: There are disclosed a (2-chloro-3-oxo-1-alkenyl)-bicyclo[3.3.0 octene derivative represented by the formula: ##STR1## wherein R.sup.1 represents --CH.sub.2 CH.sub.2 CH.sub.2 COOR.sup.5, --CH.sub.2 CH.sub.2 --O--CH.sub.2 COOR.sup.5, --CH.dbd.CHCH.sub.2 COOR.sup.5 or --CH.sub.2 CH.sub.2 C.tbd.C--COOR.sup.5 group where R.sup.5 in the groups represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms; R.sup.2 represents a hydrogen atom, an acyl group having 1 to 7 carbon atoms, a tri(1 to 7 carbon atoms)-hydrocarbylsilyl group or a group forming an acetal bonding with an oxygen atom of a hydroxy group; R.sup.

Abstract: New ketolactones of the formula I ##STR1## wherein R.sup.1 is H, alkyl having 1-6 C atoms or aryl having 6-14 C atoms andR.sup.2 and R.sup.3 together are an O atom or together are a bond,and salts thereof,can be used as intermediate products in the preparation of prostaglandin derivatives.

Abstract: The present invention provides a novel process for reducing 15-keto prostaglandin intermediates. This process stereospecifically reduces these 15-keto intermediates using sodium borohydride and ceriumtrichloride, yielding a predominance of the 15.alpha. epimer.

Abstract: Disclosed herein is an improved process for preparing 1RS-3'RS epimer of aminated phthalideisoquinolines represented by the general formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen atom or a lower alkoxy group, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are independently hydrogen atom, amino group or a lower alkoxy group with at least one of R.sup.3 -R.sup.6 being amino group, and R.sup.7 is a lower alkyl group. The improvement comprises, after having reduced a mixture of epimers of corresponding nitro compounds of the general formula (I) wherein the amino group is replaced by nitro group into the amino compounds (I), treating said amino compound at a temperature in the range of 20.degree.-100.degree. C. in an aliphatic lower alcohol in the presence of an alkali to epimerize 1RS-3'SR epimer of said amino compound into said 1RS-3'RS epimer thereof.

Abstract: A novel process for preparing a 3-phenacylidene phthalide of the general formula (II) ##STR1## which comprises reacting a halogenating reagent with a 2-carboxydibenzoylmethane.The 2-carboxydibenzoylmethane can be inexpensively prepared, so that the 3-phenacylidene phthalides which are useful as a growth regulant for plants and a safering agent to reduce herbicidal injury to plants can be readily obtained economically in high yield.

Abstract: A compound of the formula ##STR1## and intermediates useful in preparing same.

Abstract: A process for the production of (1R,Cis)-4-acetyl-6, 6-dimethyl-3-oxabicyclo-(3.1.0.)-hex-2-one of the formula: ##STR1## which involves reacting (1R,Cis)-4,7,7-trimethyl-3-oxabicyclo-(4.1.0.)-hept-4-en-2-one of the formula: ##STR2## with bromine at a temperature of from 0.degree. C. to 25.degree. C. and treating the brominated reaction mixture at ambient temperature with water, an aqueous solvent solution or an aqueous base solution.

Abstract: A compound of the formula ##STR1## and intermediates useful in preparing same.

Abstract: Arenes, such as benzoic acid and substituted benzoic acids, are readily thallated by thallium(III) compounds such as the trifluoroacetate and subsequently reacted with palladium chloride and simple olefins, dienes, allylic halides, vinyl halides, vinyl esters, or unsaturated cyclopropanes or unsaturated cyclobutanes to give isocoumarins.

Abstract: 7-fluoro-16-substituted 15-hydroxy PGI.sub.2 compounds which have saturated bond of the 13 position and which are useful as blood platelet anti-aggregating agents.

Abstract: The present invention relates to intermediates of the general formula: ##STR1## (wherein Y and Z, which may be the same or different, each represents a trans-vinylene group or an ethylene group, R.sup.2 represents a hydrogen atom or a methyl or ethyl group, R.sup.3 represents a single bond or an alkylene group of 1 to 5 carbon atoms, R.sup.4 represents an alkyl group of 1 to 8 carbon atoms, a cycloalkyl group of 4 to 7 carbon atoms unsubstituted or substituted by at least one alkyl group of 1 to 8 carbon atoms or a phenyl or phenoxy group unsubstituted or substituted by at least one halogen atom, trifluoromethyl group or alkyl group of 1 to 4 carbon atoms, R.sup.5 represents a hydroxy- protecting group which can be removed in acidic conditions and W.sup.1 represents a group of the formula: --COOR.sup.1, --CON(R.sup.6).sub.2, --CH.sub.2 OR.sup.5 or --CH(OR.sup.7)CH.sub.2 OR.sup.5 (in which R.sup.1 represents a hydrogen atom or an alkyl group of 1 to 12 carbon atoms, the groups R.sup.

Abstract: A process for producing prostacyclins of the formula ##STR1## wherein the symbol G.sup.1, R.sup.1, R.sup.2, R.sup.31 and R.sup.41 are as defined in claim 1,which comprises reacting 5,6-dehydroprostaglandins F.sub.2 of the formula ##STR2## wherein the symbol G, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined in claim 1,with a mercury (II) compound in an inert organic solvent in the presence of tri(C.sub.1 -C.sub.6)alkylamine, treating the reaction product with a boron hydride compound, and if necessary, subjecting the reaction product to deprotecting reaction, hydrolysis reaction, or salt-forming reaction.This process is industrially advantageous process for the preparation of prostacyclin and its derivatives.

Abstract: The prostacyclins 7-fluoro-6,9-epoxy-16-substituted-15-hydroxyprost-[4 or 5,13]-dienoic acids and esters useful as anti-secretory agents, blood pressure lowering agents, anti-ulcerogenic agents, anti-hypertensive agents, bronchodilation agents and for combating gastro-hyperacidity and as anti-blood platelet aggregating agents.

Abstract: A novel process for the preparation of sulfonic acid esters containing a lactonic ring comprising compounds in the trans form in the 4- and 5-positions having (4SR,5RS), (4S,5R) or (4R,5S) configuration of the formula ##STR1## wherein Z is selected from the group consisting of alkyl of 1 to 4 carbon atoms and cycloalkyl and monocyclic aryl optionally substituted with at least one member of the group consisting of alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, halogen and nitro and R is organic residue of an optionally chiral alcohol of the formula ROH and a process using the compounds of formula I to prepare compounds of (1RS, 4RS, 5SR), (1S, 4S, 5R) or (1R, 4R, 5S) configuration of the formula ##STR2## wherein X is selected from the group consisting of hydrogen and R useful for the preparation of insecticidally active esters.

Abstract: Hydroquinones of the formula ##STR1## wherein X is the residue of a 5- or 6-membered ring, R.sub.1 is hydrogen, alkyl or aryl, R.sub.1,R.sub.3, R.sub.4 and R.sub.5 are hydrogen or alkyl and R.sub.6 is hydrogen or a group of the formula ##STR2## wherein X and R.sub.1 are as defined above, are of use as protected developing agents in photographic silver halide material.

Abstract: The present invention concerns novel phthalidyl esters of arylalkanoic acids having improved pharmacological properties in respect to the corresponding arylalkanoic acids having analgesic and anti-inflammatory activity, as well as pharmaceutical compositions containing them as active ingredients. The invention further relates to a method for improving the pharmacological properties of said arylalkanoic acids having analgesic and anti-inflammatory activity, by introducing, through an ester bond, a phthalidyl group.

Abstract: Lactones of the formula ##STR1## wherein R is hydrogen or a CX.sub.3 group, and each X is a chlorine or bromine atom, are converted to the known cis-3-(2,2-dihalovinyl)-2,2-dimethylcyclopropanecarboxylic acids or lower alkyl esters, from which pyrethroid insecticides are obtained.

Abstract: Racemic carboxylic acids are resolved into their enantiomers using optically active enantiomers of four lactones as resolving agents. The four lactones are 2,3-isopropylidene-ribonic acid-1,4-lactone, 1,2-isopropylideneglucofuranurono-3,6-lactone, 2-hydroxy-3,3-dimethyl-1,4-butyrolactone and 3,4-isopropylidene-arabino-1,5-lactone. Novel diastereoisomeric esters of the acids with the lactones are disclosed.

Abstract: Novel 5- or 7-monohalogenated or 5,7-dihalogenated .sup.6 -PGI.sub.1 and 5- or 7-monohalogenated or dihalogenated PGI.sub.2 (except 5-monofluorinated PGI.sub.2). The novel halogenated prostacyclins are useful for controlling vascular actions and also in organ transplantation, extra-corporeal circulation and the like. The present invention also provides processes for preparing the novel halogenated prostacyclins.

Abstract: (1R,cis)-Oxyimino-substituted cyclopropanecarboxylic acids are prepared via a (1R,4R,5S)-2-acetoxy-6,6-dimethyl-4-oxo-3-oxabicyclo[3.1.0]hexane intermediate.

Abstract: (1R,cis)-Oxyimino-substituted cyclopropanecarboxylic acids are prepared via a (1R,4R,5S)-4-acetoxy-6,6-dimethyl-2-oxo-3-oxabicyclo [3.1.0]hexane intermediate.

Abstract: Novel compounds of the following general formula: ##STR1##

Abstract: An improved process for the preparation of 3-substituted thiophenes. The thiophenes are useful for the preparation of penicillins and cephalosporins.The process is for the preparation of a thiophene of formula (I): ##STR1## where R.sup.1 represents a carboxylic acid group, or an ester or amide thereof or a nitrile group; R.sup.2 represents a group suitable for use as an .alpha.-substituent in the side-chain of a penicillin or cephalosporin; which comprises treating under basic conditions a compound of formula (II): ##STR2## wherein X represents halogen or optionally functionalized hydroxyl, Y represents halogen, hydroxyl, or alkoxy; with a source of nucleophilic sulphur ionically bound to a polymeric support.

Abstract: A novel process for producing 7-alkoxycarbonyl-6,8-dimethyl-4-hydroxymethyl-1-phthalazone, and its intermediates. 7-Alkoxycarbonyl-6,8-dimethyl-4-hydroxymethyl-1-phthalazone can be obtained by reacting substituted methylenetriphenylphosphorane with 3,5-dimethyl-4-alkoxycarbonylphthalic anhydride to obtain 6-alkoxycarbonyl-5,7-dimethyl-.DELTA..sup.3,.alpha. -substituted methylenephthalide, reacting the latter with hydrazine to obtain a phthalazone derivative, hydrolyzing the latter, halogenating the hydrolyzate to obtain 7-alkoxycarbonyl-6,8-dimethyl-4-(.alpha.-halogeno-.alpha.-substituted methyl)-1-phthalazone and then directly hydrolyzing and decarboxylating the latter or, when said 7-alkoxycarbonyl-6,8-dimethyl-4-(.alpha.-halogeno-.alpha.-substituted methyl)-1-phthalazone is 7-alkoxycarbonyl-6,8-dimethyl-1-phthalazone-4-.alpha.

Abstract: The present specification provides novel analogs of carbacyclin (CBA.sub.2), 6a-carba-prostacyclin (6a-carba-PGI.sub.2), which have pronounced prostacyclin-like pharmacological activity, e.g., as platelet anti-aggregatory agents. Specifically the novel chemical analogs of CBA.sub.2 are those substituted by fluoro (C-5), alkyl (C-9), interphenylene (C-5), and methano (C-6a,9). Further provided are benzindene analogs of CBA.sub.2 and substituted forms thereof, i.e., 9-deoxy-2',9-methano (or 2',9-metheno)-3-oxa-4,5,6-trinor-3,7-(1',3'-interphenylene)-PGF.sub.1 compounds. Also provided are a variety of novel chemical intermediates, e.g., substituted bicyclo[3.3.0]octane intermediates, and chemical process utilizing such intermediates which are useful in the preparation of the novel CBA.sub.2 analogs.

Abstract: Novel intermediates for production of insecticidal cis-3-(2,2-disubstituted-ethenyl)-2,2-dimethylcyclopropanecarboxylates, processes for preparing the intermediates, and processes for preparing the final product insecticides via a novel bicyclic lactone intermediate are described and exemplified.

Abstract: Compounds of formula (III): ##STR1## and esters, amides and pharmaceutically acceptable salts thereof, wherein A.sup.1 is hydrogen or methyl;A.sup.2 is hydrogen or methyl;n is 1, 2 or 3; andR is hydrogen, chlorine, bromine, hydroxy, nitro, amino or trifluoromethyl,are useful as anti-hyperglycaemic agents and/or anti-obesity agents.