Ciba-geigy Corporation

Novartis Ag

Novartis Corporation

Solvias Ag

Destiny Pharma Limited

Novartis Finance Corporation

Merck & Cie

Benoit Pugin

Felix Spindler

Manfred Muller

Heidi Landert

William Guy Love

William Rhys-Williams

Derek Brundish

Rudolf Moser

Viola Groehn

Adriano Indolese

Andreas Pfaltz

Gerardo Ramos

Hans R Muller

Matthias Lotz

Adrian Wyss

Raphael Aardoom

Xiang Feng

Richard Breitschuh

Verena Gisin

Yann Ribourdouille

Giorgio Pioda

Xiang Dong Feng

Balamurugan Ramalingam

Xiangdong Feng

William Love

Bjoern Gschwend

Weiping Chen

Compounds of the formula (I) in the form of a mixture of predominantly one diastereomer or in the form of pure diastereomers,Z-Q-P*RR&#x2003;&#x2003;(I),wherein:

Bidentate chiral ligands for use in catalytic asymmetric addition reactions

A compound of formula I: wherein X, X, X, X, Y, Y, Y, Yand Z have meanings given in the description, and metallated forms of such compounds, which are useful in the treatment of medical conditions for which a photodynamic compound is indicated. Pharmaceutical formulations and methods of treatment of a medical condition for which a photodynamic agent is indicated are also disclosed. Sterilizing solutions comprising a compound of the invention, and the use thereof, are also disclosed.

Porphyrin derivatives and their use in photodynamic therapy

Process for the preparation of tetrahydropterin and tetrahydropterin derivatives by hydrogenating pterin and pterin derivatives with hydrogen in the presence of a hydrogenating catalyst, in which the hydrogenation is carried out in a polar reaction medium and metal complexes that are soluble in the reaction medium are employed as the hydrogenation catalysts. The process is suited to the hydrogenation, particularly asymmetric hydrogenation, of folic acid, folic acid salts, folic acid esters, folic acid ester salts or dihydroforms thereof, with the proviso that in the event of using folic acid, carboxylic acid salts thereof or dihydroforms thereof the reaction medium is aqueous, and in the event of using folic acid esters, folic acid ester salts or dihydroforms thereof the reaction medium is an alcohol. The process opens up straightforward access to achiral and chiral pterin derivatives.

Process for the preparation of optically pure tetrahydropterins and derivatives, and specifically of optically pure tetrahydrofolic acid and derivatives thereof, by stereospecific hydrogenation

The invention relates to 1,2-ferrocenyldiphosphines which contain a functional group in the 1&prime; position either directly or via a bridging group, and also a process for their preparation. The compounds are important for transition metal complexes containing d-8 metals such as Rh, Ru, Pd or Ir. These transition metal complexes are widely used in the hydrogenation of organic double or triple bonds, in particular olefinic double bonds and carbon-heteroatom double bonds. The complexes are particularly suitable for enantioselective hydrogenation using chiral ferrocenyldiphosphines and corresponding prochiral unsaturated compounds. Ferrocenyldiphosphines having a functional group in the 1&prime; position are also important intermediates for ferrocenyldiphosphine ligands and their metal complexes of d-8 metals such as rhodium, ruthenium, palladium or iridium which are bound to inorganic polymeric supports via this functional group. These metal complexes bound to an inorganic or organic support material are likewise very suitable for the hydrogenation of organic double or triple bonds.

Functionalized ferrocenyldiphosphines, a process for their preparation and their use

Chiral ferrocenyls

The invention relates to a compound of formula I ##STR1## R.sub.1 is C.sub.1 -C.sub.8 alkyl, phenyl or phenyl substituted by from 1 to 3 C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy substituents;

Dihalogenated ferrocenes and processes for the preparation thereof

Process for the preparation of substituted 3-aminobenzonitriles

The invention relates to ferrocenyldiphosphine ligands containing a silylene group, ferrocenyldiphosphines bound to inorganic or polymeric organic supports by this silylene group, their preparation and also their metal complexes with transition metals such as rhodium or iridium. The invention also relates to the use of these complexes for hydrogenating organic double or triple bonds, in particular olefinic double bonds and carbon-heteroatom double bonds. The complexes are particularly suitable for enantioselective hydrogenation using chiral diphosphines and prochiral unsaturated compounds.

Silylated ferrocenyldiphosphines, silylated ferrocenyldiphosphines bound

The invention relates to polymers having structural repeating units of at least one monomer MM which contains a hydroxyl group or a primary or secondary amine group as a functional group bonded directly or in a side chain, wherein the functional group is bonded via a bridge group Q formed by a diisocyanate to the hydroxyl group or primary or secondary amino group of an aliphatic, cycloaliphatic, heterocycloaliphatic, aromatic or heteroaromatic ditertiary diphosphine, the phosphine groups of which are bonded to a carbon chain in the 1,2-, 1,3-, 1,4- or 1,5-position relative to one another. The invention also relates to a process for their preparation and to rhodium and iridium complexes with these diphosphine ligands. Using these rhodium and iridium complexes, optically pure compounds which are valuable intermediates for the preparation of biologically active ingredients, in particular in the field of pharmaceuticals and agrochemicals, can be obtained in a hydrogenation process which is likewise according to the invention. Thus, for example, it is possible to prepare from secondary amines, in particular N-carbalkoxymethylamines, 5-imidazolecarboxylic acid derivatives which have a herbicidal action and can be used for weed control (EP-A-0 207 563). The optically pure (.alpha.-aminocarboxylic acid esters are suitable for peptide syntheses. After the hydrogenation, the catalysts can easily be separated off, if appropriate purified and re-used.

Diphosphines bonded to side chains of polymers, and metal complexes

The invention relates to ferrocenyldiphosphine ligands containing a silylene group, ferrocenyldiphosphines bound to inorganic or polymeric organic supports by this silylene group, their preparation and also their metal complexes with transition metals such as rhodium or iridium. The invention also relates to the use of these complexes for hydrogenating organic double or triple bonds, in particular olefinic double bonds and carbon-heteroatom double bonds. The complexes are particularly suitable for enantioselective hydrogenation using chiral diphosphines and prochiral unsaturated compounds. The preparation of these immobilized ferrocenyldiphosphines has only been made possible by the provision of correspondingly functionalized ferrocenyldiphosphines. These compounds and their preparation are likewise novel. Accordingly, the invention also provides compounds of the formula I ##STR1## in which R.sub.1 is C.sub.1 -C.sub.8 alkyl, phenyl or phenyl substituted by from 1 to 3 C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxyalkoxy groups; R.sub.2, R.sub.3, R.sub.10 and R.sub.11 are, independently of one another, C.sub.1 -C.sub.12 alkyl, C.sub.5 -C.sub.12 cycloalkyl, phenyl, C.sub.5 -C.sub.12 cycloalkyl substituted by C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy, or phenyl substituted by from one to three C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, --SiR.sub.4 R.sub.5 R.sub.6, halogen, --SO.sub.3 M, --CO.sub.2 M, --PO.sub.3 M, --NR.sub.7 R.sub.8, --[+NR.sub.7 R.sub.8 R.sub.9 ]X.sup.- or C.sub.1 -C.sub.5 fluoroalkyl groups; or the groups --PR.sub.2 R.sub.3 and --PR.sub.10 R.sub.11 are each, independently of one another, a radical of the formula II, IIa, IIb or IIc ##STR2## and R.sub.4, R.sub.5 and R.sub.6 are, independently of one another, C.sub.1 -C.sub.12 alkyl or phenyl;

Compounds of formula I ##STR1## wherein R.sub.1 denotes identical or different radicals and is linear or branched C.sub.1 -C.sub.12 alkyl, unsubstituted C.sub.5 -C.sub.6 cycloalkyl or C.sub.5 -C.sub.6 cycloalkyl which is substituted by C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy, or is phenyl or benzyl, or both substituents R.sub.1 of a group (R.sub.1).sub.2 P are o,o'-diphenylene, R.sub.2 is hydrogen, linear or branched C.sub.1 -C.sub.12 alkyl, phenyl or benzyl, R.sub.3 is C.sub.1 -C.sub.12 alkylene, R.sub.4 is C.sub.2 -C.sub.18 alkylene, phenylene or benzylene, and R.sub.5 is C.sub.1 -C.sub.6 alkyl or phenyl, can be applied to solid carriers, such as silica gel or aerosils, and complexed with rhodium or iridium compounds. These materials are heterogeneous and separable catalysts for the asymmetrical hydrogenation of prochiral compounds containing carbon double bonds or carbon/hetero atom double bonds, for example ketones and imines.

Diphosphines containing silane groups, immobilized diphosphines and the

Compounds of formula I ##STR1## wherein R.sub.1 denotes identical or different radicals and is linear or branched C.sub.1 -C.sub.12 alkyl, unsubstituted C.sub.5 -C.sub.6 cycloalkyl or C.sub.5 -C.sub.6 cycloalkyl which is substituted by C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy, or is phenyl or benzyl, or both substituents R.sub.1 of a group (R.sub.1).sub.2 P are o,o-diphenylene, R.sub.2 is hydrogen, linear or branched C.sub.1 -C.sub.12 alkyl, phenyl or benzyl, R.sub.3 is C.sub.1 -C.sub.12 alkylene, R.sub.4 is C.sub.2 -C.sub.18 alkylene, phenylene or benzylene, and R.sub.5 is C.sub.1 -C.sub.6 alkyl or phenyl, can be applied to solid carriers, such as silica gel or aerosils, and complexed with rhodium or iridium compounds. These materials are heterogeneous and separable catalysts for the assymetrical hydrogenation of prochiral compounds containing carbon double bonds or carbon/hetero atom double bonds, for example ketones and imines.

Diphosphines containing silane groups, immobilized diphosphins and the

Compounds where a solid carrier material which contains diphosphine rhodium or iridium complexes fixed on the surface thereof, of which the carrier material has the formula IV or IVa: ##STR1## wherein Y denotes two monoolefin ligands or a diene ligand, M is Ir(I) or Rh(i), Z is --Cl, --Br or -I, A.crclbar. is the anion of an oxyacid or complex acid, T is a solid carrier material, r is 0, 1 or 2, and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as defined in claim 1. These materials are heterogeneous and separable catalysts for the asymmetrical hydrogenation of prochiral compounds containing carbon double bonds or carbon/hetero atom double bonds, for example ketones and imines.

Diphosphines containing silane groups, immobilised diphosphines and the

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Benoit Pugin