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    Process for making chiral 1,4-disubstituted piperazines
    6.
    发明授权
    Process for making chiral 1,4-disubstituted piperazines 失效
    制备手性1,4-二取代哌嗪的方法

    公开(公告)号：US07256289B2

    公开(公告)日：2007-08-14

    申请号：US11147055

    申请日：2005-06-07

    申请人： Ivo Ladislav Jirkovsky ,  Joseph Zeldis ,  Gregg Brian Feigelson

    发明人： Ivo Ladislav Jirkovsky ,  Joseph Zeldis ,  Gregg Brian Feigelson

    IPC分类号： C07D405/04

    CPC分类号： C07D487/10 ,  C07B2200/07 ,  C07C229/12 ,  C07C309/06 ,  C07D319/18

    摘要： A process for a stereoselective preparation of novel chiral nitrogen mustard derivatives useful in synthesizing optically active 1,4-disubstituted piperazines of formula: wherein R, Ar, and Q are defined as set forth herein, and intermediate compounds therefor. The 1,4-disubstituted piperazines act as 5HT1A receptor binding agents useful in the treatment of Central Nervous System (CNS) disorders. The intermediate compounds of Formula II and IV as set forth herein are also included.

    摘要翻译： 用于立体选择性制备新型手性氮芥衍生物的方法，其用于合成下式所示的光学活性1,4-二取代哌嗪：其中R，Ar和Q如本文所述定义，及其中间体化合物。 1,4-二取代的哌嗪作为可用于治疗中枢神经系统（CNS）障碍的5HT1A受体结合剂。 还包括本文所述的式II和IV的中间体化合物。

    Aryloxy-alkyl-dialkylamines
    9.
    发明授权
    Aryloxy-alkyl-dialkylamines 失效
    芳氧基 - 烷基 - 二烷基胺

    公开(公告)号：US06242605B1

    公开(公告)日：2001-06-05

    申请号：US09458316

    申请日：1999-12-10

    申请人： Panolil Raveendranath ,  Joseph Zeldis ,  Galina Vid ,  John R. Potoski ,  Jianxin Ren ,  Silvio Iera

    发明人： Panolil Raveendranath ,  Joseph Zeldis ,  Galina Vid ,  John R. Potoski ,  Jianxin Ren ,  Silvio Iera

    IPC分类号： C07D23702

    CPC分类号： C07D295/088 ,  C07C217/48

    摘要： The present invention provides compounds useful in the synthesis of biologically active compounds, and processes for their production, the compounds having the formula: wherein: R1 and R2 are, independently, selected from H; C1-C12 alkyl or C1-C6 perfluorinated alkyl; X represents a leaving group; A is 0 or S; m is an integer from 1 to 3, preferably 2; R3, R4, R5, and R6 are independently selected from H, halogen, —NO2, alkyl, alkoxy, C1-C6 perfluorinated alkyl, OH or the C1-C4 esters or alkyl ethers thereof, —CN, —O—R1, —O—Ar, —S—R1, —S—Ar, —SO—R1, —SO—Ar, —SO2—R1, —SO2—Ar, —CO—R1, —CO—Ar, —CO2—R1, or —CO2—Ar; and Y is selected from a) the moiety: wherein R7 and R8 are independently selected from the group of H, C1-C6 alkyl, or phenyl; or b) an optionally substituted five-, six- or seven-membered saturated, unsaturated or partially unsaturated heterocycle or bicyclic heterocycle containing up to two heteroatoms selected from the group consisting of —O—, —NH—, —N(C1C4 alkyl)—, —N═, and —S(O)n—.

    摘要翻译： 本发明提供了可用于合成生物活性化合物的化合物及其制备方法，具有下式的化合物：其中：R 1和R 2独立地选自H; C1-C12烷基或C1-C6全氟化烷基; X表示离去基团; A为0或S; m为1〜3的整数，优选为2; R 3，R 4，R 5和R 6独立地选自H，卤素，-NO 2，烷基，烷氧基，C 1 -C 6全氟烷基，OH或其C 1 -C 4酯或其烷基醚，-CN，-O-R 1， O-Ar，-S-R 1，-S-Ar，-SO-R 1，-SO-Ar，-SO 2 -R 1，-SO 2 -Ar，-CO-R 1，-CO-Ar，-CO 2 -R -CO 2 -Ar; 并且Y选自a）部分：其中R 7和R 8独立地选自H，C 1 -C 6烷基或苯基; 或b）任选取代的五元，六元或七元饱和的不饱和或部分不饱和的杂环或双环杂环，其含有至多两个选自-O - ， - NH - ， - N（C 1 -C 4烷基） - ， - N =和-S（O）n - 。

    Process for making chiral 1,4-disubstituted piperazines
    10.
    发明申请
    Process for making chiral 1,4-disubstituted piperazines 审中-公开
    制备手性1,4-二取代哌嗪的方法

    公开(公告)号：US20080058543A1

    公开(公告)日：2008-03-06

    申请号：US11891062

    申请日：2007-08-08

    申请人： Joseph Zeldis ,  Gregg Feigelson ,  Ivo Jirkovsky

    发明人： Joseph Zeldis ,  Gregg Feigelson ,  Ivo Jirkovsky

    IPC分类号： C07C309/63 ,  C07C229/02

    CPC分类号： C07D487/10 ,  C07B2200/07 ,  C07C229/12 ,  C07C309/06 ,  C07D319/18

    摘要： A process for a stereoselective preparation of novel chiral nitrogen mustard derivatives useful in synthesizing optically active 1,4-disubstituted piperazines of formula: wherein R, Ar, and Q are defined as set forth herein, and intermediate compounds therefor. The 1,4-disubstituted piperazines act as 5HT1A receptor binding agents useful in the treatment of Central Nervous System (CNS) disorders.

    摘要翻译： 用于立体选择性制备新型手性氮芥衍生物的方法，其用于合成下式所示的光学活性1,4-二取代哌嗪：其中R，Ar和Q如本文所述定义，及其中间体化合物。 1,4-二取代的哌嗪作为可用于治疗中枢神经系统（CNS）障碍的5HT1A受体结合剂。