Laboratorios Del Dr. Esteve S.a.

Laboratories Del Dr. Esteve S.a.

Matthias Lormann

Helmut Heinrich Buschmann

Antoni Torrens Jover

Stefan Dahmen

A process is described for the preparation of a precursor alcohol of Cizolirtine, (&#xb1;)-2-[phenyl(1-methyl-1H-pyrazol-5-yl)methoxy]-N,N-dimethylethanamine and its enantiomers. The process involves the asymmetric addition of a metalated phenyl reagent to a pyrazolcarbaldehyde in the presence of a chiral ligand to yield chiral alcohols. The chiral alcohols are further O-alkylated to yield Cizolirtine or its enantiomers.

Process for obtaining Cizolirtine and its enantiomers

A process is described for the preparation of a precursor alcohol of (&#xb1;)-2-[thienyl(1-methyl-1H-pyrazol-5-yl)methoxy]-N,N-dimethyletanamine and in general for thienylazolylalcoxyethanamines and their enantiomers. The process involves asymmetric addition of a metalated thienyl reagent to a pyrazolcarbaldehyde in the presence of a chiral ligand to yield chiral alcohols. The chiral alcohols are further O-alkylated to yield the corresponding pharmaceutically active thienylazolylalcoxyethanamines.

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Aachen, Germany

Matthias Lormann