Abstract: The invention relates to a method for producing 2-chloro-5-chloromethyl-1,3-thiazol from compounds of formula (I), wherein X means Cl, —OR, —SR or NR2, R being H or a suitable protective group; Y means H or Cl and Z means Cl or O, the compounds of formula (I) having at most one double bond between C* and C″ or between C″ and Z, on the condition that the bond between C″ and Z is a double bond when Z is the same as O and a single bond when Z is the same as Cl; with the following intermediate stage: A1) reacting 2,3-dichloropropanal with rhodanide and acetalising to 3-chloro-1,1-dialkoxy-2-isothiocyanato-propane or a2) reacting 2,3-dichloropropanal with thiourea to form a mixture of the hydrochlorides of the compounds N-[[5-(2-aminothiazol)yl]methyl]thiourea and [5-(2-aminothiazol)yl]methylthioformamidine and splitting to obtain the corresponding thiol or amine or b) reacting a compound of formula (I) wherein X means OR, SR or NR2, Y means clorine and Z

Abstract: The invention relates to a method for producing 2-oxindoles from the corresponding isatines of formula (I), wherein R can be H, CH3, phenyl or benzyl and R1 can be H, C1-C4-alkyl, C1-C4-alkoxy, phenyl phenoxy, halogen, amino, nitro or hydroxy. Said isatines are converted by means of hydrazine hydrate in a polar solvent at a temperature of 15 to 185° C. to form a corresponding isatine hydrazone which directly undergoes further reaction to form the corresponding 2-oxindole of formula (II) by adding diazabicyclooctane and/or diazabicycloundecane and/or ethyldiisopropylamine as a catalyst in temperatures of 100 to 185° C., whereby the produced reaction water is distilled off. According to formula (II), R and R1 have the aforementioned definitions. The 2-oxindole is isolated from the reaction mixture by distilling off the solvent and by means of crystallisation.

Abstract: The invention relates to a method for producing 2-oxindoles from the corresponding isatines of formula (I), wherein R can be H, CH3, phenyl or benzyl and R1 can be H, C1-C4-alkyl, C1-C4-alkoxy, phenyl, phenoxy, halogen, amino, nitro or hydroxy. Said isatines are converted by means of hydrazine hydrate in a polar solvent at a temperature of 15 to 185° C. to form a corresponding isatine hydrazone which directly undergoes further reaction to form the corresponding 2-oxindole of formula (II) by adding diazabi-cyclooctane and/or diazabicycloundecane and/or ethyldiisopropylamine as a catalyst in temperatures of 100 to 185° C., whereby the produced reaction water is distilled off. According to formula (II), R and R1 have the aforementioned definitions. The 2-oxindole is isolated from the reaction mixture by distilling off the solvent and by means of crystallisation.

Abstract: The invention relates to a method for producing optionally substituted aliphatic, aromatic or heteraromatic aldehydes of formula (I), whereby the R represents a C1-C20 Alkyl radical, an aromatic or heteraromatic radical Ar which can optionally be substituted once or on a number of occasions by OH, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 carboxylic acids or ester containing 1-6 C atoms in the ester part, phenyl, halogen, SO3H, NO2, NR1R2 or SR1 whereby R1 and R2 can be independently H, phenyl or C1-C6 alkyl. The invention is characterised by a compound of formula (II) wherein R has the above meaning, a) is diazotized in an acidic medium, at a temperature of between −10 −+100 ° C. by a diazoation reagent and is transformed into the corresponding hydroxy carboxy acid whereby b) is transformed, by means of oxygen, into the appropriate aldehyde of formula (I) in the presence of a metal, the salt thereof, oxide or hydroxide as a catalyst.

Abstract: A method for the production of substituted aromatic aldehydes or ketones and optionally substituted heteroaromatic aldehydes or ketones of formula (I) by reacting a compound of formula (II) in a suitable solvent in the presence of a carbonyl compound of formula (III), optionally in the presence of oxygen at a normal pressure or high temperature and at temperatures of 5-200° C.

Abstract: Process for preparing glyoxylic esters or their hydrates in which a water-soluble salt of a maleic or fumaric monoester or a mixture thereof is reacted with ozone in aqueous solution at temperatures of from 0 to 50.degree. C., and the corresponding glyoxylic ester or its hydrate is isolated from the resulting reaction mixture.

Abstract: Process for the preparation of carboxylic acid succinimidyl esters by reaction of N-hydroxysuccinimide with a carboxylic acid and a halophosphoric acid ester of the formula ##STR1## in which R.sub.1 and R.sub.2 are identical or different and are a C.sub.2 - to C.sub.6 -alkyl radical or a phenyl radical, or R.sub.1 and R.sub.2 together form a C.sub.6 -aryl radical, in the presence of a base in a diluent at a temperature of 0.degree. C. up to 100.degree. C. and isolation of the corresponding carboxylic acid succinimidyl ester.

Abstract: A process for the preparation of carboxylic acid succinimidyl esters by reaction of N-hydroxysuccinimide with a carboxylic acid and a halophosphoric acid ester of the formula ##STR1## is desired, in which R.sub.1 and R.sub.2 are identical or different and are a C.sub.2 - to C.sub.6 -alkyl radical or a phenyl radical, or R.sub.1 and R.sub.2 The process is carried out in the presence of a base in a diluent at a temperature of 0.degree. C. up to 100.degree. C. with isolation of the corresponding carboxylic acid succinimidyl ester.

Abstract: This invention relates to compounds having selective LTB.sub.4 antagonist properties. Therapeutic compositions comprising said compounds and methods for the treatment of disorders involving LTB.sub.4 agonist-mediated activity utilizing said compositions wherein the compounds are described by the formula ##STR1## wherein R.sub.4, X, R, Y, R', Q, m and n are herein defined, and pharmaceutically acceptable salts thereof.

Abstract: Process for the preparation of 5-arylhydantoins by reaction of an allantoin acid alkyl ester with an aryl compound in a concentrated inorganic acid at temperatures from room temperature to 150.degree. C., with or without a phase transfer agent.

Abstract: This invention relates to compounds having selective LTB.sub.4 antagonist properties, compositions comprising said compounds and methods for the treatment of disorders involving LTB.sub.4 agonist-mediated activity utilizing said compositions wherein the compounds are described by the general formula ##STR1## and pharmaceutically acceptable salts thereof.

Abstract: Compounds of the structural formulae ##STR1## and their pharmaceutically acceptable salts, esters and amide derivatives, in which R.sup.1 and R.sup.2, independently of one another, denote hydrogen or pharmaceutically acceptable groups which have 1 to 10 carbon atoms and are bonded to the remaining part of the molecule via carbon-carbon single bonds, and in which R.sup.3, R.sup.4 and R.sup.5, independently of one another, denote pharmaceutically acceptable groups which have 1 to 10 carbon atoms and are bonded to the remaining part of the molecule via carbon-carbon single bonds, are useful antibiotics.The trisubstitution by three groups R.sup.3, R.sup.4 and R.sup.5, which are bonded via carbon-carbon single bonds, results in a noticeable increase in the hydrolysis stability and thus also in the antibacterial action of axapenemcarboxylic acids.