Hoechst Aktiengesellschaft

Sanofi-a Ventis Deutschland Gmbh

Aventis Pharma Deutschland, Gmbh

Sanofi

Wolfgang Holla

Gerhard Beck

Reinhold Keller

Berndt Kulitzscher

Thomas Stuedemann

Christoph Tappertzhofen

Bernhard Kammermeier

Wolfgang Laux

Robert J H Scheffer

Rolf-Ludwig Hoerlein

Matthias Beller

Gerhard Breipohl

Merten Schlingmann

Manfred Schudok

Manfred Schneider

Dieter Wullbrandt

Martin Hofrichter

Heiner Jendralla

Gerd Fulling

Frank Zocher

Stephane Mutti

Bernd Junker

Jochen Hachtel

Andreas Burgard

Christophe Salagnad

Volker Derdau

Bernd Napierski

Claus-Jügen Maier

Rolf Hoerlein

Jens Atzrodt

Lorenz Neubert

Dirk Michalik

Jurgen Michalowsky

Heinz-Peter Rebenstock

Stephanie Keil

Marzena Poraj-Kobielska

Glenn Groebe

Martin Sandvoss

Johannes Heidrich

Katrin Scheibner

Jan Kiebist

Stéphane Mutti

The present invention relates to a process for deuteration of amines in the alpha and/or beta position of the N-atom by using a deuterium source and a Ruthenium(II) based catalyst.

Process for the preparation of deuterated compounds containing N-alkyl groups

The invention is related to a process for preparing compounds of the formula IV by means of conversion of aromatic aldehydes of the formula I using &#x3b1;-ketoximes of the formula II via N-oxides of the formula III to halomethyloxazoles of the formula IV, wherein R, R, R, R, R, R, R, R, X, X, X, o, n1 and n2 are as defined herein.

Method for the production of oxazoles by condensing aromatic aldehydes with &#x3b1;-ketoximes to N-oxides and then reacting the same with activated acid derivatives

The invention relates generally to a process for preparing diarylcycloalkyl derivatives of the formula (I). wherein the respective R-group substituents are defined herein. These compounds of formula (I) are activators for peroxisome proliferator-activated receptors (PPAR activators) which are useful in the therapeutic treatment of a number of diseases and disorders of the central nervous system such as multiple sclerosis, Parkinson's Disease, psychiatric disorders and the like. The present invention is a novel process for preparing PPAR activators of the formula (I) which do not have the disadvantages of the processes known in the prior art. In particular, a process is provided with which the PPAR activators of formula (I) can be prepared in a suitable enantiomeric excess, i.e. high enantioselectivity, without the need for subsequent chiral chromatography.

Method for the production of diarylcycloalkyl derivatives

The present invention is comprised of improved methods in the preparation of oxazoles which results in higher yields with less impurities and contaminants. Oxazoles constitute valuable intermediates in the synthesis of pharmaceutically active substances such as, for example peroxisome proliferator activated receptor (PPAR) agonists which are pharmaceutical actives which can have a positive influence on both lipid and glucose metabolism.

Method for the preparation of oxazoles by condensing aromatic aldehydes with &#x3b1;-ketoximes to form n-oxides and reacting same with activated acid derivatives

A process is described for preparing chiral, nonracemic, cis-configured 1,3-disubstituted cyclohexanols of the formula (I) where the radicals are as defined, by means of enzymatic optical resolution.

Process for preparing the enantiomeric forms of cis-configured 1,3-cyclohexanediol derivatives

The present invention relates to a process for the preparation of acetyl-amidiniophenylalanyl-cyclohexylglycyl-pyridinioalaninamides of the formula I, in which the anions X are physiologically acceptable anions, and their analogs, which are effective inhibitors of the blood coagulation factor Xa and which can be used, for example, for preventing thromboses. The process according to the invention comprises the coupling of 2-[2-acetylamino-3-(4-amidinophenyl)propionylamino]-2-cyclohexylacetic acid, which is obtained from 2-[2-acetylamino-3-(4-cyanophenyl)acryloylamino]-2-cyclohexylacetic acid by asymmetric hydrogenation and conversion of the cyano group into the amidine, or a salt thereof, with a 3-(2-amino-2-carbamoylethyl)-1-methylpyridinium salt or a salt thereof. The invention furthermore provides starting materials and intermediates for this process, processes for their preparation and acetyl-(S)-4-amidiniophenylalanyl-(S)-cyclohexylglycyl-(S)-(1-methyl-3-pyridinio)alaninamide as ditosylate salt.

Process for the preparation of acetyl-amidiniophenylalanyl-cyclohexylglycyl-pyridinioalaninamides

The present invention relates to a process for the preparation of the enantiomeric forms of 2-substituted 2-(2,5-dioxoimidazolidin-1-yl)acetic acid derivatives of the formula I,wherein R, Rand Rhave the meanings given in the claims, by stereodifferentiating conversion of mixtures of the enantiomers with the aid of enzymes.

Process for the preparation of the enant iomeric forms of 2-substituted 2- (2, 5-dioxoimidazolidin-1yl) -acetic acid derivatives

The invention relates to a method for producing optically pure compounds of 3(R)- and 3(S)-hydroxy-1-methyl-4-(2,4,6-trimethoxyphenyl)-1,2,3,6-tetrahydro-pyridine or its carboxylic acid esters by reacting the enantiomer mixtures stereoselectively, using an enzyme.

Method for enzymatic enantiomer-separation of 3(r)- and 3(s)-hydroxy-1-methyl-4-(2,4,6-trimethoxyphenyl)-1,2,3,6-tetrahydro-pyridine or its carboxylic acid esters

Method for producing S-alkyl(aryl)-substituted imidazol derivatives

The present invention relates to a process for the preparation of chiral, nonracemic compounds of the formula I ##STR1## in which R.sup.1 and R.sup.2 have the meanings indicated in claim 1 and which are useful intermediates for the preparation of pharmaceutical active compounds in which, for resolution, a salt is formed from the racemic compound of the formula I and a chiral, nonracemic amino compound. It furthermore relates to compounds of the formula I and esters thereof.

Process for the preparation of chiral, nonracemic

Process for the resolution of rac-2-oxotricyclo�2.2.1.0.sup.3,5 !heptane-7-carboxylic acid esters using lipase from candida. Compounds of the formula I ##STR1## in which R.sup.1 has the meanings mentioned, may be obtained in isomerically pure form from enantiomer mixtures or racemic mixtures by reacting the compound of the formula I in the presence of a lipase or esterase from porcine liver, porcine pancreas, bovine pancreas or from microorganisms such as Candida, Pseudomonas, Mucor, Rhizopus and Aspergillus, or proteases from Bacillus in the presence of water and, if desired, a cosolvent and separating from one another the esters and acids present in the solution obtained.

Process for the enzymatic separation of enantiomers of

Process for the stereoselective synthesis of 3-substituted

A process for highly regioselective esterification and ester cleavage on unsaturated sugar compounds with the aid of lipases and esterases, and products which can be prepared by this process. Highly regioselective esterifications and ester cleavages can be carried out on unsaturated sugar compounds with the aid of lipases and esterases. Lipases from microorganisms or from the pancreas and liver of animals are preferably used.

Unsaturatd sugar compounds

Process for highly regioselective esterification and ester cleavage on

It has been possible to show for a first time with the process according to the invention that the synthesis of glyco conjugates is possible by direct linkage of sugars with serine, serine derivatives and serine peptides with the aid of glucosidases.

Process for the glycosidase-catalyzed synthesis of glyco conjugates

Growing community of inventors

Kelkheim, Germany

Wolfgang Holla