Abstract: Aliphatic alpha,omega-aminonitriles are prepared by partial hydrogenation of aliphatic alpha,omega-dinitriles at elevated temperatures and superatmospheric pressure in the presence of a base and of a hydrogenation catalyst, by carrying out the hydrogenation in the presence of ammonia and lithium hydroxide or of a compound which gives lithium hydroxide during the hydrogenation.

Abstract: A process for hydrocyanation of an aliphatic monoethylenically unsaturated compound, in which the ethylenic double bond is not conjugated to any other unsaturated group in the molecule, or a monoethylenically unsaturated compound in which the ethylenic double bond is conjugated to an ester group, which process uses a catalyst composition comprising a zero-valent and a multidentate phosphite ligand in the presence of a Lewis acid promoter.

Abstract: A method of producing tris(pentafluorophenyl)borane or its ether complex, using pentafluorobenzene as the source of the pentafluorophenyl group. The process comprises reacting pentafluorobenzene with an organo metallic compound (II) of the formula R.sub.2-n MgX.sub.n, wherein n denotes a real number of 0 or 1, X denotes a halogen atom and R denotes a hydrocarbon group of 1 to 10 carbon atoms. The reaction is carried out in an ether solvent at a temperature not less than 25.degree. C. The resulting pentafluorophenylmagnesium compound has the formula (C.sub.6 F.sub.5).sub.2-n MgX.sub.n (III), wherein n denotes a real number of 0 or 1 and X denotes a halogen atom. The pentafluorophenylmagnesium compound of the formula (III) is next reacted with a borane compound of the formula BX.sub.3, wherein X denotes a halogen atom. The reaction is carried out at a temperature in the range of 0.degree. C. to 250.degree. C., preferably 60.degree. C. to 250.degree. C.

Abstract: Aliphatic alpha,omega-aminonitriles are prepared by partial hydrogenation of aliphatic alpha,omega-dinitriles at elevated temperatures in the presence of a catalyst in the gas phase by a process which comprises carrying out the hydrogenation with a catalyst based on at least one metal selected from the group consisting of nickel, cobalt, ruthenium and rhodium and with the proviso that the catalyst is not a powder.

Abstract: Process for the preparation of 5,6-dihydroxyindole, wherein the compound of formula: ##STR1## in which R' denotes a hydrogen atom or an optionally substituted benzyl radical, is subjected either to the action of hydrogen under pressure or to a hydrogen transfer operation, in a solvent medium and in the presence of a hydrogenation catalyst.

Abstract: Novel proline derivatives of the following formula (I) ##STR1## wherein each symbol is as defined in the specification, which specifically inhibit prolyl endopeptidase activity and can be used for the prevention and/or treatment of dementia and amnesia as agents which act directly on the central symptoms of dementia.

Abstract: The subject of the invention is the compounds of formula I ##STR1## in which Ar.sub.1 represents naphtyl, phenyl, quinolyl or isoquinolyl optionally substituted;Ar.sub.2 represents a phenyl or thienyl optionally substituted;R.sub.1, R.sub.2 and R'.sub.2 are independently of each other, H or (C.sub.1 -C.sub.4)alkyl;R.sub.1 represents nothing and N is attached to Ar.sub.2, and optionally R.sub.2 and R'.sub.2 form a double bond; or R.sub.1 or R.sub.2 is attached to Ar.sub.2 and represents a (C.sub.1 -C.sub.3)alkylene;R.sub.3 and R.sub.4, which are identical or different, represent H, (C.sub.1 -C.sub.4)alkyl or form, with the nitrogen atom to which they are attached, a (C.sub.5 -C.sub.7) saturated heterocycle selected from pyrrolidine, piperidine and hexahydroazepine;Z.sub.1 represents a (C.sub.1 -C.sub.12)alkylene, optionally interrupted or extended by a (C.sub.5 -C.sub.7)cycloalkyl or phenyl;Q.sub.1 represents methyl, amino, alkoxycarbonylamino, alkylamino, dialkylamino, a (C.sub.5 -C.sub.

Abstract: A method of preparing an .alpha.-cyanoacrylate ester of a desired alcohol includes the steps ofpreparing a compound which is an .alpha.-selenoaryl-.alpha.-cyanopropionate ester of the desired alcohol,oxidizing said .alpha.-selenoaryl-.alpha.-cyanopropionate ester to the corresponding selenoxide,eliminating arylselenic acid from the selenoxide to produce said .alpha.-cyanoacrylate ester, andseparating said .alpha.-cyanoacrylate ester from the selenic acid.At temperatures of about 0.degree. C. or higher, the elimination step occurs concurrently with the oxidizing step using a peroxide or ozone oxidizing agent. The desired cyanoacrylate ester is obtained in good yield and very high purity. The method can be used to prepare difficult to synthesize plural functional cyanoacrylate monomers and mono- cyanoacrylate monomers regardless of alcohol chain length.

Abstract: Certain compounds have been synthesized and found to be effective inhibitors of phospholipase A.sub.2 (PLA.sub.2), and thereby useful in the treatment of intestinal cholesterol absorption and the disease states arising therefrom, such as hypercholesterolemia and coronary artery disease.

Abstract: The invention is directed to 3-aminopyrroles of formula I, which are largely new, to methods for the preparation and to their use as medicinal agents and preparations, as well as to anti-convulsive or analgesic preparations containing these 3-aminopyrroles.Disubstituted and monosubstituted amino groups are claimed as 3-amino substituents.The invention pursues the objective of developing largely new 3-aminopyrroles, which have CNS activity, particularly ones which anti-convulsive or analgesic properties, as well as methods for their preparation and their use as medicinal preparations.Pursuant to the invention, the synthesis is carried out by cyclizing open-chain precursors, such as aminoacrylic acid derivative, or by modifying pyrroles.

Abstract: Novel processes and intermediates useful for the manufacture of the Wittig ester salts are disclosed. The Wittig ester salts are known as important CS building blocks for the manufacture of various polyenecarboxylic acid esters in the field of carotenoid chemistry.

Abstract: Disclosed is a novel process for the preparation and separation of cyclopropanecarbonitrile (CPCN) from cyclopropropanecarboxaldehyde (CPCA) using a combination of three process steps. The process involves the steps of (1) reacting (CPCA) with hydroxylamine base in the presence of water to obtain CPCA oxime, (2) contacting the CPCA oxime of step (1) with formic acid to obtain CPCN, and (3) contacting the mixture comprising CPCN formed in step (2) with a base to obtain a mixture comprising an organic phase containing CPCN and an aqueous phase. The reactants and intermediates involved in each step are used within certain defined ratios.

Abstract: A process for making 2,6-difluorobenzonitrile, comprising reacting 2,6-dichlorobenzonitrile with a substantially anhydrous metal fluoride at a temperature between about 160.degree. C. and about 300.degree. C. and in the presence of a phase transfer catalyst, which is typically a polyether, tetra-substituted phosphonium salt, tetra-substituted ammonium salt, and cryptand, but in the absence of a solvent. After taking off the product the resulting mixture may be recycled into the reactor for the next reaction cycle. Upon build-up of tars in the reaction process, the invention includes the separation of catalyst from the tars and the recycle thereof.

Abstract: Process for the preparation of 5,6-dihydroxyindole, wherein the compound of formula: ##STR1## in which R' denotes a hydrogen atom or an optionally substituted benzyl radical, is subjected either to the action of hydrogen under pressure or to a hydrogen transfer operation, in a solvent medium and in the presence of a hydrogenation catalyst.

Abstract: This invention provides a novel compound TAN-1813 having farnesyltransferase-inhibitory, cell growth-inhibitory, and anti-tumor activities; its production; farnesyltransferase-inhibiting agent; anti-tumor agent; pharmaceutical composition comprising a compound TAN-1813; and a novel microorganism capable of producing said compound.

Abstract: This invention relates to the novel compounds and pharmaceutical compositions of Formulas (I) and (II).This invention also relates to a method of treating or reducing inflammation in a mammal in need thereof, which comprises administering to said mammal an effective amount of a compound or composition of Formula (I) or (II).

Abstract: A method for the enantioselective reduction of prochiral ketones using catalytic amounts of tetrahydroindeno[1,2-d][1,3,2] oxazaboroles of formula II is disclosed. ##STR1## The oxazaboroles can be generated in situ from the corresponding cis-1-amino-2-indanols or imino indanols (III) ##STR2## Novel compounds of formulas II and III are also disclosed.

Abstract: The invention relates to a method of preparing an optically active cyanohydrin carboxylic acid ester from an optically active cyanohydrin of opposite configuration, wherein said starting cyanohydrin is converted with a carboxylic acid in the presence of a dialkyl azodicarboxylate and a triarylphosphine.The invention also relates to a method of preparing an optically active cyanohydrin of opposite configuration by a subsequent solvolysis of the ester obtained under conservation of the configuration.

Abstract: The invention provides novel compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2, which can be the same or different are H or OH, R.sub.3 is ##STR2## wherein R.sub.4 and R.sub.5, which can be the same or different are H or an alkyl group of 1 to 4 carbon atoms, and their non-toxic pharmaceutically acceptable salts and esters and mixtures thereof, which compounds include metabolites of toremifene and exhibit valuable pharmacological properties as oestrogenic, anti-oestrogenic, and progestanic agents.

Abstract: A Process for Preparing L-(-)-carnitine is disclosed which comprises acylating D-(+)-carnitinenitrile or D-(+)-carnitineamide to their respective acyl derivatives which, via acid hydrolysis, yield D-(+)-carnitine which is converted to the lactone of L-(-)-carnitine. The lactone when in base yields L-(-)-carnitine.