公开(公告)号：EP1674458A1

公开(公告)日：2006-06-28

申请号：EP04380274.3

申请日：2004-12-27

申请人： LABORATORIOS DEL DR. ESTEVE, S.A.

发明人： Torrens Jover, Antoni ,  Buschmann, Helmut ,  Heller, Detleff ,  Drexler, Hans Joachim

IPC分类号： C07D231/12

CPC分类号： C07D231/12

摘要： A process is described for the preparation of a precursor alcohol of Cizolirtine, (±)-2-[phenyl(1-methyl-1 H -pyrazol-5-yl)methoxy]- N,N- dimethylethanamine and its enantiomers, it comprises the asymmetric reduction of a prochiral ketone in the presence of a chiral ruthenium (II) catalyst system comprising at least a bidentate phosphorous-containing ligand and a diamine ligand to render chiral alcohols. The chiral alcohols are further O-alkylated to render the corresponding pharmaceutically active ethanamines.

摘要翻译： 描述了制备Cizolirtine，（±）-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前体醇的方法，其包含 在手性钌（II）催化剂体系存在下不对称还原前手性酮，所述手性钌（II）催化剂体系包含至少二齿含磷配体和二胺配体以形成手性醇。 手性醇进一步被O-烷基化以得到相应的药学活性乙胺。

公开(公告)号：EP1674465A1

公开(公告)日：2006-06-28

申请号：EP04380275.0

申请日：2004-12-27

申请人： LABORATORIOS DEL DR. ESTEVE, S.A.

发明人： Torrens Jover, Antoni ,  Buschmann, Helmut H. ,  Heller, Detleff ,  Drexler, Hans Joachim

IPC分类号： C07D409/06

CPC分类号： C07D409/06

摘要： A process is described for the preparation of a precursor alcohol of (±)-2-[thienyl(1-methyl-1 H -pyrazol-5-yl)methoxy]- N , N dimethyletanamine and in general for thyenylazolylalcoxyethanamines and their enantiomers. It comprises the asymmetric reduction of a prochiral ketone in the presence of a chiral ruthenium (II) catalyst system comprising at least a bidentate phosphorous-containing ligand and a diamine ligand to render chiral alcohols. The chiral alcohols are further O-alkylated to render the corresponding pharmaceutically active ethanamines.

摘要翻译： 描述了制备（±）-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，通常用于甲烯基薁基乙氧基胺及其对映异构体。 它包括在手性钌（II）催化剂体系的存在下不对称还原前手性酮，所述手性钌（II）催化剂体系包含至少一个含二磷酸的配体和二胺配体以形成手性醇。 手性醇进一步O-烷基化以产生相应的药学活性乙胺。