Ciba Specialty Chemicals Corporation

Teva Pharmaceutical Industries Limited

Solvias Ag

Basf Se Corporation

Stephan Burkhardt

Martin Studer

Gabriele Baisch

Reinhold Öhrlein

Frank Bienewald

Hans Jürg Kirner

Nicole End

Jean-Pierre Wolf

Peter Murer

Hansjörg Grützmacher

Daniel Stein

Hans Jörg Kirner

Pascal Hayoz

Urs Lehmann

Philippe Bugnon

Kurt Dietliker

Kai-Uwe Schöning

Margherita Fontana

Reinhard Sommerlade

Bernd Lamatsch

Andreas Pfaltz

Souâd Boulmaâz

Ulrike Nettekoven

Laurent Michau

Jens Geier

Markus Scherer

Hartmut Schönberg

Christian Exner

Disclosed is a composition comprising a charged particle of volume 5 nmto 50 million nmpreferably having an inorganic core of SiO, AIO, and/or TiO, or a core essentially consisting of an organic pigment and/or pigment derivative, and a counter ion which is separable from the particle and is not covalently linked to the particle, said counter ion comprising a silicon atom which is directly bound to a carbon atom. Preferably, said charged particle comprises a dye attached to said inorganic core and said counter ion comprises a (poly)siloxane moiety linked via suitable bridge members to a quaternary, positively charged, nitrogen or phosphorus atom, or to a moiety carrying an anionic functional group. Said composition may be used e.g. in the form of a homogenous dispersion in an electrophoretic display.

Charged particles

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

The invention relates to a process for the preparation of (bis)acylphosphanes of formula I, wherein n and m are each independently of the other 1 or 2; R1 if n=1, is e.g. unsubstituted or substituted C-Calkyl or C-Calkenyl, or phenyl, R1 if n=2, is e.g. a divalent radical of the monovalent radical defined above; R2 is e.g. C-Calkyl, C-Ccycloalkyl, C-Calkenyl, mesityl, phenyl, naphthyl; R3 is one of the radicals defined under R; the process comprises the steps a) contacting e.g. elemental phosphorous [P]&#x221e;, P(Hal)with a reducing metal optionally in the presence of a catalyst or an activator in a solvent to obtain metal phosphides MeP or Me'P, wherein Me is an alkali metal and Me&#x2032; is an earth alkali metal or to obtain metal polyphosphides b) optionally adding a proton source, optionally in the presence of a catalyst or an activator to obtain metal dihydrogen phosphides MePH; c) subsequent acylation reaction with m acid halides of formula III or m carboxylic acid esters of formula IV or, in case that in formula I m=1, with one carboxylic ester of formula IV followed by one acid halide of formula III or vice versa, wherein R is the residue of an alcohol and Ris as defined above; d) alkylation reaction subsequent reaction with an electrophilic agent RHal or other electrophilic agents to obtain the compounds of formula I. An oxidation step may follow to obtain mono- and bisacylphosphane oxides or mono- and bisacylphosphane sulfides, which are used as photoinitiators. 

Process for preparing acylphosphanes and derivatives thereof

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 present invention relates to a new, selective process for the preparation of mono- and bisacylphosphanes of formula (I) n and m are each independently of the other 1 or 2; R, if n=1, is e.g. phenyl R, if n=2, is e.g. C-Calkylene or phenylene; Ris e. g. C-Calkyl, phenyl or substituted phenyl; Ris e. g. C-Calkyl, by (1) reacting a phosphorous halide of formula IIa or a phosphorous halide oxide of formula (IIb) or a phosphorous halide sulfide of formula (IIc) with an alkali metal in a solvent in the presence of a proton source; (2) subsequent reaction with m acid halides of formula (III) An oxidation step may follow to obtain mono- and bisacylphosphane oxides or mono- and bisacylphosphane sulfides. 

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 

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

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.

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Gelterkinden, Switzerland

Stephan Burkhardt