Hoechst Aktiengesellschaft

Zach System

Ppg Industries Ohio, Inc.

Roussel Uclaf

Novacta Biosystem Limited

Novacta Biosystems Limited

Jean-Claude Caille

Jean-Paul Vevert

Rainer Henning

Bernward Scholkens

Hermann J Gerhards

Adalbert Wagner

Alain Burgos

Stanislas Didierlaurent

Michelle Lorraine-Gradley

Marc Mauduit

Michelle Lorraine Gradley

This disclosure relates to the synthesis of the compound of formula (I) according to Scheme A below: in which R1, R2 and R3, which may be identical or different, represent, individually and independently, an alkyl group, characterized by an enzymatic hydrolysis reaction that involves placing the compound of formula (II) in contact with an enzyme that performs a chemoselective hydrolysis of only one of the two ester functions of the compound of formula (II) to obtain the compound of formula (I).

Method for the chemo-selective enzymatic hydrolysis if a diester compound for preparing a monoester monoacid compound

The invention provides the diastereoselective alkylation of optically active nopinone to form the compound of formula (I) according to scheme A below: in which: The compound of formula (I) is a valuable synthetic intermediate.

Process for the diastereoselective alkylation of an ether oxime of the compound nopinone and novel intermediates for the synthesis of diastereospecific 2-amino-nopinone derivatives substituted on carbon 3

A method of producing (S)-3-&lsqb;2-&lcub;(methylsulfonyl)oxy&rcub;ethoxy&rsqb;-4-(triphenylmethoxy)-1-butanol methane sulfonate using 1,3-butadiene and a ketoethanal to form an intermediate racemic mixture. The racemic mixture is resolved to remove one isomer from the reaction product mixture. Following resolution, the following steps are performed: reduce the isomer to an alcohol, react the alcohol with triphenylmethyl chloride, ozonalyze the resulting reaction product, reduce the ozonalyzed product to yield a diol and react the diol with a methane sulfonyl compound to form (S)-3-&lsqb;2-&lcub;(methylsulfonyl)oxy&rcub;ethoxy&rsqb;-4-(triphenylmethoxy)-1-butanol methane sulfonate. Alternatively, the racemic mixture may first be reduced and the resulting racemic alcohol mixture is resolved to isolate one isomer of the alcohol and the remaining process steps are followed.

Method of preparing 3-&lsqb;2-&lcub;(Methylsulfonyl)oxy&rcub;-ethoxy &rsqb;-4-(triphenylmethoxy)-1-butanol, methane sulfonate

Novel pyrimidine derivatives of the formula ##STR1## represents: either a group: ##STR2## or a group: ##STR3## having angiotensin II inhibiting activity.

Pyrimidine derivatives

The invention relates to compounds of the formula ##STR1## in which X, Y and Z are identical or different and are N or CR.sup.2, L is an alkylene radical, q is 0 or 1, and A is the radical of a fused heterobicyclic compound. The invention furthermore relates to a process for preparing the said compounds, agents containing these, and the use thereof for angiotensin II receptors.

Substituted imidazoles

The invention relates to compounds of the formula I ##STR1## in which X, Y and Z are identical or different and are N or CR.sup.2, R.sup.1 and R.sup.2 are as defined in the description, L is an alkylene radical, q is 0 or 1, and A is the radical of a fused heterobicyclic compound. The invention furthermore relates to a process for preparing the said compounds, agents containing these, and the use thereof in the treatment of high blood pressure.

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Angers, France

Jean-Claude Caille