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 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.
描述了一种制备(±)-2-[
噻吩基(1-甲基-1H-
吡唑-5-基)甲氧基]-N,N-二甲基
乙胺前体醇的过程,以及
噻吩基
吡唑基醇和它们的对映体的一般制备方法。该过程涉及将
金属化的
噻吩试剂不对称加到
吡唑醛中,在手性
配体存在下生成手性醇。这些手性醇进一步进行O-烷基化,生成相应的具有药用活性的
噻吩基
吡唑基醇
乙胺。