公开(公告)号：US20060142589A1

公开(公告)日：2006-06-29

申请号：US11041667

申请日：2005-01-24

申请人： Antoni Torrens Jover ,  Helmut Buschmann ,  Detleff Heller ,  Hans Drexler

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

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-1H-pyrazol-5-yl)methoxy]-N,N-dimethylethanamine and its enantiomers. The process involves the asymmetric reduction of a prochiral ketone in the presence of a chiral ruthenium (II) catalyst system including at least a bidentate phosphorous-containing ligand and a diamine ligand to yield chiral alcohols. The chiral alcohols are further O-alkylated to yield 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异构体的前体醇的方法。 该方法包括在手性钌（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）催化剂体系至少包含二齿含磷配位体和二胺配体以产生手性醇。 手性醇进一步O-烷基化以产生相应的药学活性乙胺。

公开(公告)号：US06979742B1

公开(公告)日：2005-12-27

申请号：US11041639

申请日：2005-01-24

申请人： Antoni Torrens Jover ,  Helmut H. Buschmann ,  Detleff Heller ,  Hans Joachim Drexler

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

IPC分类号： C07D409/06 ,  C07D231/10

CPC分类号： C07D409/06

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 more generally for thyenylazolylalcoxyethanamines and their enantiomers. The process involves 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 yield chiral alcohols. The chiral alcohols are further O-alkylated to yield 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，更通常用于甲烯基薁基乙氧基胺及其对映异构体 。 该方法包括在手性钌（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，以产生手性醇。 手性醇进一步O-烷基化以产生相应的药学活性乙胺。