公开(公告)号：JP2011055842A

公开(公告)日：2011-03-24

申请号：JP2010262040

申请日：2010-11-25

Applicant: H Lundbeck As ,  ハー・ルンドベック・アクチエゼルスカベット

Inventor： TAOKA NAOAKI ,  KATO TAKAHISA ,  YAMAMOTO SHOGO ,  YOSHIDA TAKASHI ,  TAKEDA TOSHIHIRO ,  UEDA YASUYOSHI ,  PETERSEN HANS ,  DANCER ROBERT ,  AHMADIAN HALEH ,  LYNGSO LARS OLE

IPC: C12P13/00 ,  C12P41/00 ,  C07B57/00 ,  C07C253/30 ,  C07C253/34 ,  C07C255/34 ,  C07C255/53 ,  C07C255/59 ,  C07D307/87

CPC classification number: C07B57/00 ,  C07B2200/07 ,  C07C253/30 ,  C07C253/34 ,  C07C255/34 ,  C07C255/59 ,  C07D307/87 ,  C12P7/22 ,  C12P13/001 ,  C12P13/002 ,  C12P13/008 ,  C12P13/02 ,  C12P41/007

Abstract: PROBLEM TO BE SOLVED: To provide a new method for preparation of optically active intermediates which may be used for the preparation of escitalopram. SOLUTION: There is provided a method for isolation and purification of S-enantiomer of the diol represented by formula (II), and its acylated derivative. The method includes treating the mixture of the S-enantiomer of the diol and its acylated derivative in the mixture of an organic solvent and water in the presence of an acid, and then performing liquid-liquid separation. In the formula, R is cyano group or the like; the dotted line represents a double or single bond; Hal is halogen; and Z is dimethylamino or the like. COPYRIGHT: (C)2011,JPO&INPIT

Abstract translation: 要解决的问题：提供可用于制备依他普仑的光学活性中间体的新方法。 解决方案：提供了由式（II）表示的二醇的S-对映异构体及其酰化衍生物的分离和纯化方法。 该方法包括在有机溶剂和水的混合物中在酸的存在下处理二醇的S-对映异构体及其酰化衍生物的混合物，然后进行液 - 液分离。 在该式中，R是氰基等; 虚线表示双键或单键; 卤素是卤素; Z为二甲基氨基等。 版权所有（C）2011，JPO＆INPIT

公开(公告)号：JP2010150270A

公开(公告)日：2010-07-08

申请号：JP2010032381

申请日：2010-02-17

Applicant: H Lundbeck As ,  ハー・ルンドベック・アクチエゼルスカベット

Inventor： TAOKA NAOAKI ,  KATO TAKAHISA ,  YAMAMOTO SHOGO ,  YOSHIDA TAKASHI ,  TAKEDA TOSHIHIRO ,  UEDA YASUYOSHI ,  PETERSEN HANS ,  DANCER ROBERT ,  AHMADIAN HALEH ,  LYNGSO LARS OLE

IPC: C07C253/34 ,  C12P13/00 ,  C07B57/00 ,  C07C253/30 ,  C07C255/34 ,  C07C255/53 ,  C07C255/59 ,  C07D307/87 ,  C12P41/00

CPC classification number: C07B57/00 ,  C07B2200/07 ,  C07C253/30 ,  C07C253/34 ,  C07C255/34 ,  C07C255/59 ,  C07D307/87 ,  C12P7/22 ,  C12P13/001 ,  C12P13/002 ,  C12P13/008 ,  C12P13/02 ,  C12P41/007

Abstract: PROBLEM TO BE SOLVED: To provide a method for separation of optically-active intermediates which may be useful for the production of escitalopram (S-enantiomer of citalopram). SOLUTION: There is provided a method for isolation and purification of S-enantiomer of the diol represented by formula (II) (wherein R is cyano or the like; the dotted line represents a double or single bond; Hal is halogen; and Z is dimethylamino or the like), and its acylated derivative. The method includes treating the mixture of the S-enantiomer of the diol and its acylated derivative in the mixture of an organic solvent and water in the presence of an acid, and then performing liquid-liquid distribution. COPYRIGHT: (C)2010,JPO&INPIT

Abstract translation: 待解决的问题：提供可用于生产西酞普兰（西酞普兰的S-对映异构体）的光学活性中间体的分离方法。 解决方案：提供了由式（II）表示的二醇的S-对映异构体的分离和纯化方法（其中R是氰基等;虚线表示双键或单键; Hal是卤素; Z为二甲基氨基等）及其酰化衍生物。 该方法包括在有机溶剂和水的混合物中在酸的存在下处理二醇的S-对映异构体及其酰化衍生物的混合物，然后进行液 - 液分配。 版权所有（C）2010，JPO＆INPIT