Lonza Ag

Lonza Inc.

Idorsia Pharmaceuticals Ltd

Other

Merck + Co., Inc.

Lonaz Ltd.

Martin Eyer

Jean-paul Roduit

Alain Wellig

Karin Amacker

Jean-Paul Roduit

Walter Brieden

Yves Bessard

Andreas Kiener

Georges Kalbermatten

Gerhard C Stucky

Eva Maria Urban

Christine Bernegger-Egli

Michael Petersen

Katja Berchtold

Holger Breitbach

Rudolf Fuchs

Erich Armbruster

Nicholas Shaw

Josef Schr&ouml;er

James Edward Leresche

Josef Schroer

Vitor Oliveira

Ivan Pogorelic

David Kuo

Ralf Proplesch

Klaus Heinzmann

David L Kuo

Rainer Glockler

Josef Schröer

Marcel Etzensperger

J Org Kohr

Jorg Kohr

Andreas Naepfli

The invention relates to a crystalline form of [(2R,3S,4R,5S)-1-butyl-2-(hydroxymethyl)-piperidine-3,4,5-triol, processes for the preparation thereof, pharmaceutical compositions containing such a crystalline form, and its use as a medicament, especially as glycolipid biosynthesis inhibitor.

Crystalline form of N-butyldeoxygalactonojirimycin

The invention relates to a novel process for the preparation of an aminoalcohol of the formula racemically or optically active, starting from 2-azabicyclo[2.2.1]hept-5-en-3-one, its further conversion to give the corresponding acyl derivative and its further conversion to (1S,4R)- or (1R,4S)-4-(2-amino-6-chloro-9-H-purine-9-yl)-2-cyclopentenyl-1-methanol of the formulae In the latter synthesis, the aminoalcohol is converted into the corresponding D- or L-tartrate, which is then reacted with N-(2-amino-4,6-dichloropyrimidin-5-yl) formamide of the formula to give (1S,4R)- or (1R,4S)-4-[(2-amino-6-chloro-5-formamido-4-pyrimidinyl)amino]-2-cyclopentenyl-1-methanol of the formulae and then cyclized to give the end compounds.

Process for the preparation of aminoalcohol derivatives and their further conversion to (1R, 4S)-4(2-amino-6-chloro-5-formamido-4- pyrimidinyl)-amino-2-cyclopentenyl-1-methanol

A four-step process for preparing 1-(6-methylpyridin-3-yl)-2-[4-(methylsulfonyl)phenyl]ethanone of the formula: starting from 2-methyl-5-ethylpyridine. 1-(6-Methylpyridin-3yl)-2-[4-(methylsulfonyl)phenyl]ethanone is an intermediate for preparing inhibitors.

Process for preparing 1-(6-methylpyridin-3-yl)-2-[4- (methylsulphonyl)phenyl]ethanone

The invention relates to a novel process for the preparation of an aminoalcohol of the formula racemically or optically active, starting from 2-azabicyclo[2.2.1]hept-5-en-3-one, its further conversion to give the corresponding acyl derivative and its further conversion to (1S,4R)- or (1R,4S)-4-(2-amino-6-chloro-9-H-purine-9-yl)-2-cyclopentenyl-1-methanol of the formulae In the latter synthesis, the aminoalcohol is converted into the corresponding D- or L-tartrate, which is then reacted with N-(2-amino-4,6-dichloropyrimidin-5-yl)formamide of the formula to give (1S,4R)- or (1R,4S)-4-[(2-amino-6-chloro-5-formamido-4-pyrimidinyl)amino]-2-cyclopentenyl-1-methanol of the formulae and then cyclized to give the end compounds.

Process for the preparation of aminoalcohol derivatives and their further conversion to (1R, 4S)-4(2-amino-6-chloro-5-formamido-4-pyrimidinyl)-amino-2-cyclopentenyl-1-methanol

The invention relates to a novel process for the preparation of an aminoalcohol of the formula racemically or optically active, starting from 2-azabi-cyclo[2.2.1]hept-5-en-3-one, its further conversion to give the corresponding acyl derivative and its further conversion to (1S,4R)&#x2014; or (1R,4S)-4-(2-amino-6-chloro-9-H-purine-9-yl)-2-cyclopentenyl-1-methanol of the formulae In the latter synthesis, the aminoalcohol is converted into the corresponding D- or L-tartrate, which is then reacted with N-(2-amino-4,6-dichloropyrimidin-5-yl) formamide of the formula to give (1S, 4R)- or (1R, 4S)-4-[(2-amino-6-chloro-5-formamido-4-pyrimidinyl)amino]-2-cyclopentenyl-1-methanol of the formulae and then cyclized to give the end compounds.

Process for the preparation of aminoalcohol derivatives and their further conversion to (1R,4S)-4-(2-amino-6-chloro-5-formamido-4-pyrimidinyl)-amino)-2-cyclopentenyl-1-methanol

A starting product for the preparation of COX-2 inhibitors, notably the compound 1-(6-methylpyridine-3-yl)-2-[(4-(methylsulfonyl)phenyl]ethanone of the formula (I): A method for making the compound.

1-(6-methylpyridine-3-yl)-2-[4-(methylsulphonyl) phenyl] ethanone and method for its preparation

A method for preparing pyridine-2,3-dicarboxylic acid esters of the general formula:wherein R is C-alkyl, C-cycloalkyl, aryl or arylalkyl, and Rto R, independently of one another, represent hydrogen, C-alkyl, fluorinated C-alkyl, C-alkoxy, (C-alkoxy)-C-alkyl or (C-alkoxy)carbonyl. These esters are obtained from the corresponding 2,3-dichloropyridine, the corresponding alcohol ROH and carbon monoxide in the presence of a palladium-diphosphine complex and a weak base. Pyridine-2,3-dicarboxylic acid esters are herbicides or intermediates for the preparation of herbicides.

Method for preparing pyridine-2,3-dicarboxylic acid esters

Process for the preparation of aminoalcohol derivatives and their further conversion to (1R,4S)-4-((2-amino-6-chloro-5-formamido-4-pyrimidinyl)-amino)-2-cyclopentenyl-1-methanol

Process for the preparation of arylamides of heteroaromatic carboxylic acids

Process for the preparation of aminoalcohol derivatives and their further conversion to (1R, 4S)-4-((2-amino-6-chloro-5-formamido-4-pyrimidinyl)-amino)-2-cyclopentenyl-1-methanol

A process for the preparation of arylamides of heteroaromatic carboxylic acids of the formula:

A biologically pure culture of microorganisms capable of converting RS-&agr;-piperazinecarboxamides into the corresponding R-&agr;-piperazinecarboxylic acid. R-&agr;-piperazinecarboxamides is the only nitrogen source.

Biotechnical production process of piperazine R-&agr;-carboxylic acids and piperazine S-&agr;-carboxylic acid amide

A process for preparing pyridinecarboxylic esters of the general formula:

Process for preparing pyridinecarboxylic esters

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Jean-Paul Roduit