Merck Patent Gmbh

Cardiome Pharma Corp.

Merck Patent Gesellschaft MIT Beschrankter Haftung

Eprova Ag

Merck Patent Gesellschaft MIT Beschraenkter Haftung

Correvio International Sàrl

Alfred Hedinger

Michael Wilhelm Platscher

Bertrand M C Plouvier

Doug Ta Hung Chou

Tao Sheng

Grace Jung

Anthony G M Barrett

Pirmin Ulmann

Lewis Siu Leung Choi

Marco Silvio Passafaro

Martin Kurz

Daniel Moeckli

Hans-Rudolf Muller

Hans-Rudolf Mueller

Werner Kuendig

Anthony Gm Barrett

Werner Kundig

Doug Ta Chou

Lewis Siu Choi

Betrand Mc Plouvier

Marco S Passafaro

Michael Platscher

Anthony GM Barrett

The present invention relates to crystal modifications of racemic (2R,S)- and enantiomerically pure (2R)-resp. (2S)-DOTAP chloride, to processes for the preparation thereof, and to the use thereof for the preparation of pharmaceutical compositions.

Stable crystal modifications of DOTAP chloride

Methods for the preparation of stereoisomerically substantially aminocyclohexyl ether compounds such as trans-(1R,2R)-aminocyclohexyl ether compounds and/or trans-(1S,2S)-aminocyclohexyl ether compounds as well as various intermediates and substrates are disclosed.

Synthetic process for aminocyclohexyl ether compounds

The invention relates to enantiomerically pure DOTAP chloride and stable crystal modifications of (2R,S)-, (2S)- and (2R)-DOTAP chloride, to a process for the preparation of these modifications, and to the use thereof as constituent for the preparation of medicaments.

Methods for the preparation of stereoisomerically substantially aminocyclohexyl ether compounds such as trans-(1R,2R)-aminocyclohexyl ether compounds and/or trans-(1S,2S)-aminocyclohexyl ether compounds as well as various intermediates and substrates are disclosed. 

The invention relates to stable crystal modifications of (R,S)-, (R)- and (S)-DOPC, to a process for the preparation of these modifications, and to the use thereof as constituent for the preparation of medicaments.

Stable crystal modifications of DOPC

A process for the simultaneous production of fructose and of gluconic acid from glucose-fructose mixtures and/or from invert sugar by the selective oxidation of the glucose proportion, wherein oxygen and/or air, activated by noble metal catalysts, are utilized as the oxidizing agents; the oxidation is conducted in a pH range of about 8 to 10; and the oxidation is terminated after the formation of 1 equivalent of carboxylic acid per mole of glucose employed. The thus-obtained gluconic acid can subsequently be separated from the unchanged fructose in a simple way and practically quantitatively, and can be isolated as the salt.

Process for the simultaneous production of fructose and gluconic acid

The yield of 4-methyl-5-hydroxymethyl-imidazole from the known reaction between formaldehyde and 4-methyl-imidazole can be increased greatly if the reaction is performed in a concentrated aqueous medium at pH 11-13.5, preferably 12-13.5, at a temperature of 20.degree.-60.degree. C., preferably 30.degree.-40.degree. C., with an amount of formaldehyde not exceeding 1.5 mole per mole of 4-methyl-imidazole.

Method of preparing 4-methyl-5-hydroxymethyl-imidazole

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Thayngen, Switzerland

Alfred Hedinger