PROCESS FOR OBTAINING ENANTIOMERS OF THIENYLAZOLYLALCOXYETHANAMINES

摘要

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