OPTICALLY ACTIVE DIBENZAZEPINE DERIVATIVES
    3.
    发明公开
    OPTICALLY ACTIVE DIBENZAZEPINE DERIVATIVES 有权
    光学活性的二氮杂吖庚因衍生物

    公开(公告)号:EP2264038A1

    公开(公告)日:2010-12-22

    申请号:EP09730232.7

    申请日:2009-04-08

    IPC分类号: C07D491/16 C07D317/60

    摘要: It is to provide a novel optically active dibenzazepine derivative having a high utility value as an asymmetric phase-transfer catalyst. It is an optically active 6,7-dihydro-5H-dibenzo[c,e]azepine derivative represented by the following formula (1'), (wherein R represents a divalent organic group for cross-linking the 1 st position and the 11 th position; R 1 and R 2 are the same or different, and represent a hydrogen atom, halogen atom, or organic group, or R 1 and R 2 together represent a divalent organic group; R 3' and R 4' are the same or different and represent a monovalent organic group, or R 3' and R 4' together form an organic group that forms a cyclic structure comprising an onium nitrogen atom; Ar represents a monovalent organic group; * represents optical activity, i.e., that one axially asymmetric isomer is present in excess of the other axially asymmetric isomer with respect to a bond axis that constitutes the biphenyl structure of the compound; and X - represents a counter anion).

    摘要翻译: 本发明提供作为非对称相转移催化剂具有高利用价值的新型光学活性二苯并氮杂衍生物。 它是由下式(1')表示的旋光的6,7-二氢-5H-二苯并[c,e]氮杂卓衍生物,(其中R代表用于交联第1位和第11位的二价有机基团 ; R1和R2相同或不同,表示氢原子,卤素原子或有机基团,或者R1和R2一起表示二价有机基团; R3'和R4'相同或不同并且表示一价有机基团 ,或者R3'和R4'一起形成形成包含氮原子的环状结构的有机基团; Ar表示一价有机基团; *表示光学活性,即一个轴向不对称异构体轴向超过另一个 相对于构成化合物的联苯结构的键轴的不对称异构体;并且X-表示抗衡阴离子)。

    PRODUCTION PROCESS OF OPTICALLY ACTIVE 3-QUINUCLIDINOL DERIVATIVE
    9.
    发明公开
    PRODUCTION PROCESS OF OPTICALLY ACTIVE 3-QUINUCLIDINOL DERIVATIVE 有权
    VERFAHREN ZUR HERSTELLUNG EINES OPTISCH AKTIVEN 3-CHINUCLIDINOL-DERIVATS

    公开(公告)号:EP2186812A1

    公开(公告)日:2010-05-19

    申请号:EP08829356.8

    申请日:2008-09-02

    摘要: A process is provided for efficiently producing an optically active 3-quinuclidinol derivative of high optical purity using a readily available ruthenium compound as an asymmetric reduction catalyst. This process is a process for producing an optically active 3-quinuclidinol derivative represented by the following formula (III) comprising asymmetrically hydrogenating a 3-quinuclidinone derivative represented by the following formula (I) in the presence of a ruthenium compound (II) represented by formula (II): Ru(X) (Y) (Px) n [R 1 R 2 C * (NR 3 R 4 )-A-R 5 R 6 C * (NR 7 R 8 )] (in the formulas, R represents a hydrogen atom or C7 to C18 aralkyl group and the like, X and Y represent hydrogen atoms or halogen atoms and the like, Px represents a phosphine ligand, n represents 1 or 2, R1 to R8 represent hydrogen atoms or C1 to C20 alkyl groups and the like, * represents an optically active carbon atom and A represents an ethylene group and the like).

    摘要翻译: 提供了使用容易获得的钌化合物作为不对称还原催化剂有效地制备高光学纯度的光学活性3-奎宁环醇衍生物的方法。 该方法是制备由下式(III)表示的光学活性3-奎宁环醇衍生物的方法,包括在下述式(I)表示的钌化合物(II)的存在下不对称地氢化下式(I)表示的3-奎宁环酮衍生物: 式(II):Ru(X)(Y)(Px)n [R 1 R 2 C *(NR 3 R 4)-AR 5 R 6 C *(NR 7 R 8)](式中,R表示 氢原子或C 7〜C 18芳烷基等,X和Y表示氢原子或卤素原子等,P x表示膦配体,n表示1或2,R 1至R 8表示氢原子或C 1至C 20烷基 等,*表示光学活性碳原子,A表示亚乙基等)。