Duphar International Research Bv

Chris G Kruse

Arne Van Der Gen

Johannes Brussee

Nicolaas Buizer

Wolter Ten Hoeve

Hans Wynberg

Belal Shadid

Klara M Schenk

Melle Van Der Laan

Gustaaf Jm Van Scharrenburg

Maria C Snoek

Jantje R Thiecke

Georges Langrand

Erwin G Warmerdam

The invention relates to a method for the stereoselective preparation of a hetero-bicyclic alcohol enantiomer, characterized in that a substantially pure enantiomer of the general formula ##STR1## is prepared from a compound of the general formula ##STR2## wherein the variable are as defined as in claim 1. The method comprises the following successive reaction steps:

Process for the stereoselective preparation of a hetero-bicyclic alcohol

The invention relates to an enzymatic process for the stereoselective preparation of a hetero-bicyclic alcohol enantiomer, characterized in that a substantially pure enantiomer of the general formula ##STR1## wherein X is O, S, NH, N--(C.sub.1 -C.sub.4)alkyl or CH.sub.2 ; Y.sub.1, Y.sub.2 and Y.sub.3 are each independently hydrogen or substituents selected from halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkyl, nitro and cyano;

Enzymatic process for the stereoselective preparation of a

The invention relates to a method of preparing an optically active cyanohydrin carboxylic acid ester from an optically active cyanohydrin of opposite configuration, wherein said starting cyanohydrin is converted with a carboxylic acid in the presence of a dialkyl azodicarboxylate and a triarylphosphine. The invention also relates to a method of preparing an optically active cyanohydrin of opposite configuration by a subsequent solvolysis of the ester obtained under conservation of the configuration.

Method of preparing optically active cyanohydrin derivatives

The present invention is concerned with a method for the preparation of a compound of the general formula 2 ##STR1## by reaction of a compound of the formula 3

Method of preparing aryl(homo)piperazines

The present invention is concerned with the preparation of N-substituted vicinal aminoalcohol derivatives from the corresponding hydroxyl-protected cyanohydrin derivatives by successive partial reduction, transimination using a primary amine, reduction of the resulting imine and optional removal of the hydroxyl-protecting group. The products are obtained either as a racemate or in an optically pure form, depending upon the stereochemical composition of the starting cyanohydrin derivatives. The present invention is also concerned with certain new enantiomerically pure hydroxyl-protected vicinal aminoalcohols.

Method of preparing vicinal aminoalcohols

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Weesp, Netherlands

Chris G Kruse