Isoxazoline derivatives as p n ligands
    55.
    发明申请
    Isoxazoline derivatives as p n ligands 失效
    异恶唑啉衍生物作为pn配体

    公开(公告)号:US20040171841A1

    公开(公告)日:2004-09-02

    申请号:US10485839

    申请日:2004-02-04

    IPC分类号: C07F009/653

    摘要: The invention relates to novel ligands of the phosphanylbenzothiophenyl-dihydroisoxazoline, phosphanyl-dihydrooxazolyl-indole and phosphanyl-dihydrooxazolyl-benzofuran type, especially compounds of formula I 1 and mixtures of such compounds, wherein X is oxygen, sulfur, selenium or NQ, wherein Q is unsubstituted or substituted aryl, or alkyl or substituted alkyl; n is 0, 1, 2, 3 or 4; A1 and A2 are each an organic radical capable of bonding to phosphorus, especially unsubstituted or substituted alkyl, unsubstituted or substituted aryl, unsubstituted or substituted heterocyclyl, unsubstituted or substituted cycloalkyl, or nullN(D)2 wherein D2 is alkyl or substituted alkyl; or A1 and A2 together with the bonding phosphorus atom form a ring, which may be unsubstituted or substituted; Y, Ynull, Ynull and Ynullnull are each independently of the other hydrogen or alkyl, substituted alkyl, unsubstituted or substituted aryl, or unsubstituted or substituted heterocyclyl, at least one of the radicals Y, Ynull, Ynull or Ynullnull being one of the mentioned radicals with the exception of hydrogen; and Z, when present, is a substituent, it being possible when a plurality of substituents Z is present for those substituents to be selected independently of one another, and to processes for their preparation, to novel precursors and intermediates, to complexes with the said ligands, to their preparation and to their use as catalysts in organic synthesis (especially asymmetric organic synthesis).

    摘要翻译: 本发明涉及膦酰基苯并噻吩基 - 二氢恶唑啉,膦基 - 二氢恶唑基 - 吲哚和膦基 - 二氢恶唑基 - 苯并呋喃型的新配体,特别是式I化合物及其混合物,其中X是氧,硫,硒或NQ,其中Q是 未取代或取代的芳基,或烷基或取代的烷基; n为0,1,2,3或4; A1和A2各自是能够键合到磷的有机基团,特别是未取代或取代的烷基,未取代或取代的芳基,未取代或取代的杂环基,未取代或取代的环烷基或-N(D)2,其中D 2是烷基或取代的烷基; 或A1和A2与键合磷原子一起形成环,其可以是未取代的或取代的; Y,Y',Y“和Y”'各自独立地为另一个氢或烷基,取代的烷基,未取代或取代的芳基,或未取代或取代的杂环基,基团Y,Y',Y' '或Y''是除了氢之外的所提及的基团之一; 当存在时,Z是一个取代基,当对于那些彼此独立选择的那些取代基存在多个取代基Z,并且其制备方法,新的前体和中间体与所述的 配体,它们的制备和用作有机合成(特别是不对称有机合成)中的催化剂。

    Arylpiperazines having activity at the serotonin 1A receptor
    58.
    发明授权
    Arylpiperazines having activity at the serotonin 1A receptor 失效
    具有5-羟色胺1A受体活性的芳基哌嗪

    公开(公告)号:US06645967B2

    公开(公告)日:2003-11-11

    申请号:US10022045

    申请日:2001-12-18

    IPC分类号: A61K31495

    摘要: Described herein is a method for potentiating the action of a serotonin reuptake inhibitor in increasing the availability of serotonin, norepinephrin and dopamine in the brain, by administering to a patient an effective amount of a compound of the formula wherein Ar′ is a mono or bicyclic aryl or heteroaryl radical substituted with one to three substituents selected from the group consisting of hydrogen, (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio, (C2-C6)alkenyl, (C2-C6)alkynyl, (C1-C6)alkylhalo, (C3-C8)cycloalkyl, (C3-C8)cycloalkenyl or halo; R1 is hydrogen, (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio; R2 is phenyl, naphthyl or (C3-C12)cycloalkyl substituted with one or two substituents selected from the group consisting of hydrogen (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio, (C2-C6)alkenyl, (C2-C6)alkynyl, (C1-C6)alkylhalo, (C3-C8)cycloalkyl, (C3-C8)cycloalkenyl or halo; R3 is selected from the group consisting of hydrogen (C1-C6)alkyl, (C1-C6)alkoxy, (C1-C6)alkylthio, (C2-C6)alkenyl, (C2-C6)alkynyl, (C1-C6)alkylhalo, (C3-C8)cycloalkyl, (C3-C8)cycloalkenyl or halo; X is —(C═O)—; or a pharmaceutically acceptable salt, racemate, optical isomer or solvate thereof.

    摘要翻译: 本文描述了一种增强5-羟色胺再摄取抑制剂在增加脑中5-羟色胺,去甲肾上腺素和多巴胺的可利用性的作用的方法,其通过向患者施用有效量的式I的化合物Ar'为单环或双环芳基或 被一个至三个选自氢,(C 1 -C 6)烷基,(C 1 -C 6)烷氧基,(C 1 -C 6)烷硫基,(C 2 -C 6)烯基,(C 2 -C 6) ,(C 1 -C 6)烷基卤代,(C 3 -C 8)环烷基,(C 3 -C 8)环烯基或卤素; R 1是氢,(C 1 -C 6)烷基,(C 1 -C 6)烷氧基,(C 1 -C 6) (C 1 -C 6)烷氧基,(C 1 -C 6)烷硫基(C 1 -C 6)烷基,(C 1 -C 6)烷氧基, ,(C 2 -C 6)烯基,(C 2 -C 6)炔基,(C 1 -C 6)烷基卤代,(C 3 -C 8)环烷基,(C 3 -C 8)环烯基或卤素; R 3选自氢 (C 1 -C 6)烷基,(C 1 -C 6)烷氧基,(C 1 -C 6)烷硫基,(C 2 -C 6) 6)链烯基,(C2-C6)炔基,(C1-C6)烷基卤代,(C3-C8)环烷基,(C3-C8)环烯基或卤素; X是 - (C = O) - ;或其药学上可接受的盐, 外消旋物,旋光异构体或其溶剂化物。

    Process for producing oxide with higher oxidation than alcohol
    60.
    发明申请
    Process for producing oxide with higher oxidation than alcohol 失效
    生产氧化物高于酒精的氧化物的方法

    公开(公告)号:US20030114712A1

    公开(公告)日:2003-06-19

    申请号:US09959844

    申请日:2001-11-28

    摘要: The present invention provides a process for producing an oxide from an alcohol compound, the process comprising the steps of causing silica gel to carry the alcohol compound thereon and an oxidative catalyst thereon, and oxidizing the alcohol compound in the presence of an oxidizing agent, giving an oxide higher in oxidizing degree than the alcohol compound, and also provides a process for producing an oxide from an alcohol compound, the process comprising the steps of causing silica gel to carry the alcohol compound, and subjecting the alcohol compound to an electrolytic oxidation, giving an oxide higher in oxidizing degree than the alcohol compound.

    摘要翻译: 本发明提供一种由醇化合物制备氧化物的方法,该方法包括以下步骤:使硅胶在其上载有醇化合物及其上的氧化催化剂,并在氧化剂存在下氧化醇化合物,得到 氧化度高于醇化合物的氧化物,还提供了由醇化合物制造氧化物的方法,该方法包括使硅胶携带醇化合物,并对醇化合物进行电解氧化, 产生氧化度高于醇化合物的氧化物。