A process is described for the preparation of a precursor alcohol of Cizolirtine, (±)-2-[phenyl(1-methyl-1H-pyrazol-5-yl)methoxy]-N,N-dimethylethanamine and its enantiomers, it comprises the asymmetric addition of a metalated phenyl reagent to an pyrazolcarbaldehyde in the presence of a chiral ligand to render chiral alcohols. The chiral alcohols are further O-alkylated to render Cizolirtine or its enantiomers.
描述了一种制备Cizolirtine的前体醇,即(±)-2-[苯基(1-甲基-1H-
吡唑-5-基)甲氧基]-N,N-二甲基
乙胺及其对映体的过程,包括在手性
配体存在下将
金属化的苯基试剂不对称加成到
吡唑醛中以生成手性醇。这些手性醇进一步进行O-烷基化以生成Cizolirtine或其对映体。