Sanofi-a Ventis Deutschland Gmbh

Thomas Stuedemann

Wolfgang Holla

Berndt Kulitzscher

Christoph Tappertzhofen

Wolfgang Laux

Robert J H Scheffer

Rolf-Ludwig Hoerlein

Wilfried Schwab

Heiner Jendralla

Frank Zocher

Stephane Mutti

Bernd Junker

Jochen Hachtel

Christophe Salagnad

Rolf Hoerlein

Claus-Jügen Maier

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

The invention relates to chiral Mannich bases of formula (I), chiral 1,3-amino alcohols of formula (II) derived therefrom, wherein R, R, R, Rand Rare as defined herein, and to processes for preparing Mannich salts of formula (III) containing a chiral anion Y*and compounds of formulae (I) and (II), wherein R, R, R, R, Rand Y*are as defined herein. 

Optically active &#x3b2;-aminoketones, optically active 1,3-amino alcohols and processes for preparing them

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Kelkheim, Germany

Thomas Stuedemann