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    CHIRAL REDUCTIONS OF IMINES LEADING TO THE SYNTHESES OF OPTICALLY ACTIVE AMINES
    22.
    发明申请
    CHIRAL REDUCTIONS OF IMINES LEADING TO THE SYNTHESES OF OPTICALLY ACTIVE AMINES 审中-公开
    导致光活性氨基酸合成的基因组的减少

    公开(公告)号：WO1997011934A1

    公开(公告)日：1997-04-03

    申请号：PCT/US1996015506

    申请日：1996-09-27

    Applicant: NPS PHARMACEUTICALS, INC.

    Inventor： NPS PHARMACEUTICALS, INC. ,  VAN WAGENEN, Bradford, C. ,  BARMORE, Robert, M.

    IPC: C07C209/52

    CPC classification number: C07C209/52

    Abstract: A process for preparing an R enantiomer of a compound of formula (I) wherein Me is methyl, Ar is 3-methoxyphenyl, 3-chlorophenyl, or 1-naphthyl, and X is independently selected from the group consisting of H, F, Cl, Br, I, phenyl, CF3, CF2H, CFH2, lower alkyl (e.g., Me), O-lower alkyl (e.g., OMe), OCH2CF3, OH, CN, NO2, C(O)-lower alkyl (e.g., C(O)Me), C(O)O-lower alkyl (e.g., C(O)OMe), C(O)NH-lower alkyl (e.g., C(O)NH-Me), C(O)N-lower alkyl2 (e.g., C(O)NMe2), OC(O)-lower alkyl (e.g., OC(O)Me), and NH-C(O)-lower alkyl (e.g., NH-C(O)Me), where "lower alkyl" is selected from a group consisting of 1 to 6 carbon atoms, and m is an integer between 1 and 5, by asymmetrically and enantioselectively reducing an imine with a reducing agent/chiral auxiliary agent complex so as to produce an enantiomeric excess of R enantiomer of the compound of formula (I) over the S enantiomer of the compound of formula (I). The process is especially useful to produce compounds (R)-(+)-N-[1-(3-methoxyphenyl)ethyl]-3-(2-chlorophenyl)propanamine and (R)-(+)-N-[1-(3-methoxyphenyl)ethyl]-3-(phenyl)propanamine. Enantiomeric excess of the R enantiomer over S enantiomer of greater than 65 % have been achieved.

    Abstract translation: 制备式（I）化合物的R对映异构体的方法，其中Me是甲基，Ar是3-甲氧基苯基，3-氯苯基或1-萘基，X独立地选自H，F，Cl ，Br，I，苯基，CF 3，CF 2 H，CFH 2，低级烷基（例如Me），O-低级烷基（例如OMe），OCH 2 CF 3，OH，CN，NO 2，C（O） - 低级烷基 （O）Me），C（O）O-低级烷基（例如C（O）OMe），C（O）NH-低级烷基（例如C（O）NH-Me） 低级烷基2（例如C（O）NMe 2），OC（O） - 低级烷基（例如OC（O）Me）和NH-C（O） - 低级烷基（例如NH-C（O） 其中“低级烷基”选自1至6个碳原子，m为1至5之间的整数，通过用还原剂/手性助剂络合物不对称和对映选择性还原亚胺，以产生 式（I）化合物的R对映体与式（I）化合物的S对映异构体的对映异构体过量。 该方法特别适用于制备化合物（R） - （+） - N- [1-（3-甲氧基苯基）乙基] -3-（2-氯苯基）丙胺和（R） - （+） - N- [ - （3-甲氧基苯基）乙基] -3-（苯基）丙胺。 R对映异构体超过S对映异构体的对映异构体过量已达到大于65％。

    FLUORESCENCE DETECTION APPARATUS
    23.
    发明申请
    FLUORESCENCE DETECTION APPARATUS 审中-公开
    荧光检测装置

    公开(公告)号：WO1996018115A1

    公开(公告)日：1996-06-13

    申请号：PCT/US1995015910

    申请日：1995-12-06

    Applicant: NPS PHARMACEUTICALS, INC.

    Inventor： NPS PHARMACEUTICALS, INC. ,  HAROOTUNIAN, Alec, T.

    IPC: G01T01/00

    CPC classification number: G01N21/6452 ,  C12M41/46 ,  G01N21/251 ,  G01N21/645 ,  G01N35/0099 ,  G01N2021/6463 ,  G01N2021/6484 ,  G01N2021/6493 ,  G01T7/02

    Abstract: A fluorescence analysis system detects light transmitted from wells in a sample plate. One embodiment of the system includes a single light detector. A reflector is capable of receiving light from any one of several detection emitters and of reflecting the light toward the light detector. One reflector includes a prism which is mounted on a stepping motor. The prism is selectively rotated so that it faces each detection emitter in turn. The light from several wells in a row is directed toward the light emitter by rotating the prism to face, one-by-one, each of the emitters corresponding to the wells. The detection emitters include one end of an optical fiber bundle. The other end of each bundle is positioned near the wells, with each bundle positioned by a different well to carry light from that well to the corresponding emitter. A collimating lens is positioned between each detection emitter and the rotating prism to focus light from the emitter onto the prism. A baffle is positioned between the light detector and the prism. Light from a xenon arc excitation lamp is carried by optical fiber bundles toward the sample wells. A computerized controller coordinates light detection with the activities of an automated liquid handling system.

    Abstract translation: 荧光分析系统检测从样品板中的孔传输的光。 该系统的一个实施例包括单个光检测器。 反射器能够从几个检测发射器中的任何一个接收光并将光反射到光检测器。 一个反射器包括安装在步进电机上的棱镜。 选择性地旋转棱镜，使其相反地面向每个检测发射器。 通过将棱镜旋转到与孔相对应的每个发射器一个接一个地将来自连续的几个井的光引向光发射器。 检测发射体包括光纤束的一端。 每个束的另一端位于孔附近，每个束由不同的阱定位，以将来自该阱的光携带到相应的发射器。 准直透镜位于每个检测发射器和旋转棱镜之间，以将来自发射器的光聚焦到棱镜上。 挡板位于光检测器和棱镜之间。 来自氙弧激发灯的光由光纤束向样品阱承载。 计算机控制器通过自动化液体处理系统的活动来协调光检测。

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