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
乙胺的前体醇的方法,以及一般的
噻吩基氮杂
环醇醚
乙胺及其对映体。该过程涉及在手性
配体的存在下,将
金属化
噻吩试剂不对称地加入到
吡唑醛中,以产生手性醇。然后,手性醇被进一步O-烷基化,以产生相应的具有药用活性的
噻吩基氮杂
环醇醚
乙胺。