Ciba Specialty Chemicals Corporation

Novartis Ag

Teva Pharmaceutical Industries Limited

Solvias Ag

Basf Se Corporation

Sandoz Ag

Martin Studer

Stephan Burkhardt

Gabriele Baisch

Reinhold Öhrlein

Frank Bienewald

Peter Baumeister

Urs Siegrist

Hans Jürg Kirner

Nicole End

Frank Bachmann

Gunther Schlingloff

Josef Dannacher

Cornelia Makowka

Peter Weingartner

Grit Richter

Beat Freiermuth

Hans Jörg Kirner

Peter Herold

Paul Adriaan Van Der Schaaf

Kai-Uwe Schöning

Adriano Indolese

Andreas Pfaltz

Hans-Peter Jalett

Vadiraj Subbanna Ekkundi

Vilas N Mumbaikar

Ulrike Nettekoven

Niranjan Paingankar

Stefan Burkhardt

Christian Exner

Stefan Burckhardt

The invention relates to novel synthesis methods for the preparation of statin derivatives, which methods proceed by way of a key intermediate of formula I wherein X is halogen, acyloxy, activated hydrocarbyloxy, activated hydrocarbylthio or &#x2014;N(CH)OCH, Ris a hydroxy-protecting group and Ris a carboxy-protecting group, and, as well as to the compound of formula I, to further new intermediates and methods for their preparation by Friedel-Crafts acylation.

Process for the preparation of intermediates useful in the synthesis of statin derivatives

Process for the preparation of intermediates useful in the synthesis of statin derivatives especially 7-amino-3.5-dihydroxyhepanoic acid derivatives and intermediates thereof

The invention relates to novel synthesis methods for the preparation of the intermediates, which are suitable for the preparation of statin derivatives, especially to novel synthesis methods of the intermediate of formula VI wherein Rand Rare each independently of the other hydrogen or a hydroxy-protecting group or together are a bridging hydroxy-protecting group, and Ris a carboxy-protecting group, which methods are carried out by conversion of the intermediate of formula XIX wherein Rand Rare each independently of the other hydrogen or a hydroxy-protecting group, and Ris a carboxy-protective group. 

Process for the preparation of 7-amino syn 3,5-dihydroxy heptanoic acid derivatives via 6-cyano syn 3,5-dihydroxy hexanoic acid derivatives

Synthesis methods for the preparation of intermediates which are suitable for the preparation of statin derivatives, and especially to synthesis methods for the intermediate of formula (VI) wherein R' and R&#x2032; are each independently of the other hydrogen or hydroxy-protecting group, or together are a bridging hydroxy-protecting group; and Ris a carboxy-protecting group. 

Process for the preparation of 7-amino syn 3,5-dihydroxy heptanoic acid derivatives, intermediates thereof and methods for their preparation

The invention relates to synthesis methods for the preparation of statin derivatives, which methods proceed by way of a key intermediate of formula I wherein X is halogen, acyloxy, activated hydrocarbyloxy, activated hydrocarbylthio or N(CH)OCH, Ris a hydroxy-protecting group, and Ris a carboxy-protecting group, and, as well as to the compound of formula I, to further intermediates and methods for their preparation by Friedel-Crafts acylation. 

Process for the preparation of intermediates useful in the synthesis of statin derivatives especially 7-amino 3,5-dihydroxy heptanoic acid derivatives, and intermediates thereof

The invention relates to novel synthesis methods for the preparation of the intermediates, which are suitable for the preparation of statin derivatives, especially to novel synthesis methods of the intermediate of formula VI wherein R' and R&#x2032; are each independently of the other hydrogen or a hydroxy-protecting group or together are a bridging hydroxy-protecting group, and Ris a carboxy-protecting group, which methods are carried out by conversion of the intermediate of formula XVI wherein R&#x2032; and R&#x2032; are each independently of the other hydrogen or a hydroxy-protecting group, R* and R** are each independently of the other hydrogen or an amide-protecting group, and Ris a carboxy-protecting group; which methods proceed to further new intermediates and methods for their preparation 

Process for preparation of 7-amino syn 3,5-dihydroxy heptanoic acid derivatives, intermediates thereof and methods for their preparation

The invention relates to novel synthesis methods for the preparation of the intermediates, which are suitable for the preparation of statin derivatives, especially to novel synthesis methods of the intermediate of formula VI wherein Rand Rare each independently of the other hydrogen or a hydroxy-protecting group or together are a bridging hydroxy-protecting group, and Ris a carboxy-protecting group, which methods are carried out by conversion of the intermediate of formula XIX wherein Rand Rare each independently of the other hydrogen or a hydroxy-protecting group, and Ris a carboxy-protective group 

Disclosed is a process for the preparation of a compound of formula wherein wherein R, Rand n are as defined above, in the presence of a nickel or cobalt catalyst.

Process for the preparation of phenethylamine derivatives

The present invention relates to novel processes for the preparation of optically active 3-aminocarboxylic acids and their esters, in particular processes for the preparation of optically active compounds of the formula IA or IBas free bases or as acid addition salts thereof, in which the radicals are as defined in the description; in particular using the catalytic hydrogenation of olefinic precursors in the presence of platinum on alumina as a catalyst and the removal of chiral auxiliary groups from salt precursors; and novel process sections in the route for their synthesis, and processes for the preparation of biologically, in particular pharmacologically, active compounds, which comprise the novel processes.

Processes for the preparation of 3-aminocarboxylic acids and their esters

Diastereoselective hydrogenation of 1,3-hydroxyketones

Process for enantioselectively hydrogenating prochiral ketones to (S)-alcohols using platinum catalysts in the presence of cinchonines or quinidines as modifiers and in the presence of hydrogen, which is characterized in that the modifiers used are cinchonines unsubstituted in the 3-position, 3-ethylidenyl- or 9-methoxycinchonines or derivatives thereof in which the quinoline ring is replaced by other rings.

Hydrogenation of prochiral ketones

A process for the heterogeneous and enantioselective hydrogenation of prochiral organic &agr;-keto compounds with platinum as the catalyst in the presence of a soluble or immobilized chiral aromatic nitrogen base with at least one basic nitrogen atom adjacent to stereogenic carbon atoms, whereby prochiral &agr;-ketoacetals are hydrogenated to optically active &agr;-hydroxyacetals.

Production of optically active &agr;-hydroxyacetals

Optically active &agr;-hydroxyethers are prepared from prochiral &agr;-ketoethers by heterogeneous hydrogenation using platinum catalysts in the presence of a chiral nitrogen base in high chemical and optical yields, since this type of hydrogenation selectively hydrogenates only one diastereomer virtually to completion. The yields may be substantially increased by adding a solid, strong base which has a racemizing effect on the non-hydrogenatable diasteromer.

Preparation of optically active &agr;-hydroxyethers

The present invention provides a process for inhibiting the re-absorption of migrating dyes in the wash liquor, comprising introducing into a wash liquor containing a peroxide-containing detergent, from 0.5 to 150 mg per liter of wash liquor, of one or more manganese containing compounds.

Fabric care method

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Basel, Switzerland

Martin Studer