Rhone-poulenc Rorer S.a.

Dsm Fine Chemicals Austria Nfg Gmbh & Co. Kg

Dsm Fine Chemicals Austria Gmbh

Chemie Linz Gesellschaft M.b.h.

Dsm Chemie Linz Gmbh

Wolfram Hendel

Christian Burger

Antonia Praus

Engelbert Kloimstein

Peter Pochlauer

Norbert Dereu

Gerald Summer

Harald Poschko

Richard Labaudiniere

Anita Lamplmayr

Klaus Reiter

Eduard Perndorfer

Ulfried Felfer

Karl Heinz Giselbrecht

Klaus Fitzinger

Sylvia Krich

Karl Schwendinger

Kurt Haidinger

Antonia Viehbock

The invention relates to a method for producing 2-chloro-5-chloromethyl-1,3-thiazol from compounds of formula (I), wherein X means Cl, &mdash;OR, &mdash;SR or NR , 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&Prime; or between C&Prime; and Z, on the condition that the bond between C&Prime; 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: A ) reacting 2,3-dichloropropanal with rhodanide and acetalising to 3-chloro-1,1-dialkoxy-2-isothiocyanato-propane or a ) reacting 2,3-dichloropropanal with thiourea to form a mixture of the hydrochlorides of the compounds N-&lsqb;&lsqb;5-(2-aminothiazol)yl&rsqb;methyl&rsqb;thiourea and &lsqb;5-(2-aminothiazol)yl&rsqb;methylthioformamidine and splitting to obtain the corresponding thiol or amine or b) reacting a compound of formula (I) wherein X means OR, SR or NR , Y means clorine and Z means oxygen with thiourea to produce the compound of formula (V), or c) reacting a compound of formula (I), wherein X means OR, SR or NR , Y means chlorine and Z means oxygen with ammoniumdithiocarbamate or ammoniumthiocarbamate, to produce the compound (VIa) or (VIb); d) converting 1,2,3-trichloropropane to the corresponding thiazolidine and then dehydrogenating or e) converting 1,3-dichloro-prop-1-ene to the corresponding epoxide and then reacting said epoxide with thiourea (e ) or ammoniumdithiocarbamate or ammoniumthiocarbamate (e ).

Method for producing 2-chloro-5-chloromethyl-1,3-thiazol

The invention relates to a method for producing 2-oxindoles from the corresponding isatines of formula (I), wherein R can be H, CH , phenyl or benzyl and R can be H, C -C -alkyl, C -C -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&deg; 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&deg; C., whereby the produced reaction water is distilled off. According to formula (II), R and R have the aforementioned definitions. The 2-oxindole is isolated from the reaction mixture by distilling off the solvent and by means of crystallisation.

Method for producing oxindoles

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.

Process for preparing glyoxylic esters and their hydrates

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.

Process for the preparation of carboxylic acid succinimidyl esters

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.

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.

Substituted quinolyl compounds exhibiting selective leukotriene B.sub.4

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.

Process for the preparation of arylhydantoins

Substituted bicyclic bis-aryl compounds exhibiting selective leukotriene

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Leonding, Austria

Wolfram Hendel