Process for preparation of 1,5-diaminonaphthalenes
    83.
    发明申请
    Process for preparation of 1,5-diaminonaphthalenes 失效
    制备1,5-二氨基萘的方法

    公开(公告)号:US20030176722A1

    公开(公告)日:2003-09-18

    申请号:US10312852

    申请日:2003-01-02

    Abstract: In a process where an ortho-alkylnitrobenzene derivative and a vinyl compound as starting materials are used to prepare a 1,5-diaminonaphthalene derivative via a 4-(2-nitrobenzene)propane derivative and a 5-nitro-1-tetralone derivative, the ortho-alkylnitrobenzene derivative and a vinyl compound having an electron withdrawing group such as an acrylonitrile derivative and an acrylate may be reacted in the presence of a base to provide an aromatic nitro compound. An aromatic nitro compound such as 4-(2-nitrobenzene)butanonitrile thus obtained may be cyclized to safely, cost-effectively and selectively provide a 5-nitro-1-tetralone derivative without forming any isomer. Furthermore, from the 5-nitro-1-tetralone derivative, a 1,5-diaminonaphthalene derivative may be prepared without forming any isomer.

    Abstract translation: 在使用原烷基硝基苯衍生物和乙烯基化合物作为原料的方法中,通过4-(2-硝基苯)丙烷衍生物和5-硝基-1-四氢萘酮衍生物制备1,5-二氨基萘衍生物, 正烷基硝基苯衍生物和具有吸电子基团的乙烯基化合物如丙烯腈衍生物和丙烯酸酯可以在碱的存在下反应以提供芳族硝基化合物。 如此获得的芳族硝基化合物如4-(2-硝基苯)丁腈可以环化以安全,成本有效地选择性地提供5-硝基-1-四氢萘酮衍生物而不形成任何异构体。 此外,从5-硝基-1-四氢萘酮衍生物可以制备1,5-二氨基萘衍生物而不形成任何异构体。

    Process for the preparation of terbinafine
    85.
    发明授权
    Process for the preparation of terbinafine 失效
    制备特比萘芬的方法

    公开(公告)号:US06515181B2

    公开(公告)日:2003-02-04

    申请号:US10085699

    申请日:2002-02-28

    CPC classification number: C07C209/68 C07C211/27

    Abstract: A process for the preparation of terbinafine which comprises the reaction of tert-butylacetylene with a compound of formula (II) characterized in that the reaction is carried out in the presence of copper (I) salts and of a base, in the absence of palladium.

    Abstract translation: 一种制备特比萘芬的方法,其包括叔丁基乙炔与式(II)化合物的反应,其特征在于反应在不存在钯的情况下在铜(I)盐和碱的存在下进行 。

    Process for converting stereoisomers of sertraline into sertraline
    86.
    发明授权
    Process for converting stereoisomers of sertraline into sertraline 失效
    将舍曲林的立体异构体转化为舍曲林的方法

    公开(公告)号:US06506940B1

    公开(公告)日:2003-01-14

    申请号:US09709812

    申请日:2000-11-10

    Abstract: A process for converting the cis (1R, 4R), trans (1S, 4R), and trans (1R, 4S) stereoisomers of sertraline into sertraline comprises, starting with an initial reaction mixture which contains at least one of these stereoisomers, converting the sertraline stereoisomers into an imine form of sertraline. The imine form of sertraline is then reduced so that sertraline and at least one sertraline stereoisomer byproduct is produced in the reaction mixture. The sertraline is then recovered from the reaction mixture, e.g., by fractional crystallization (followed by resolution of sertraline from the cis (1R, 4R) stereoisomer, if necessary). The reaction mixture is then recycled through the same steps so that sertraline is produced from its stereoisomers in an asymptotic yield.

    Abstract translation: 将舍曲林的顺式(1R,4R),反式(1S,4R)和反式(1R,4S)立体异构体转化为舍曲林的方法包括,从含有至少一种这些立体异构体的初始反应混合物开始, 舍曲林立体异构体转化为亚胺形式的舍曲林。 然后减少舍曲林的亚胺形式,使得在反应混合物中产生舍曲林和至少一种舍曲林立体异构体副产物。 然后从反应混合物中回收舍曲林,例如通过分步结晶(如果需要的话从顺式(1R,4R)立体异构体中分离出舍曲林)。 然后将反应混合物通过相同的步骤循环使得舍曲林以其渐进收率从其立体异构体产生。

    Racemization of optically active amines
    87.
    发明申请
    Racemization of optically active amines 失效
    光学活性胺的外消旋化

    公开(公告)号:US20020120166A1

    公开(公告)日:2002-08-29

    申请号:US10012344

    申请日:2001-12-12

    Abstract: Optically active amines of the formula I 1 where R1 and R2 are different and R1, R2, R3 are alkyl, cycloalkyl, arylalkyl, aryl, heteroaryl and heterocyclic radicals and R3 may also be hydrogen (H), with the radicals being able to bear substituents selected from the group consisting of alkyl, cycloalkyl, alkoxy, aryloxy, amino, alkylamino and dialkylamino, are racemized by reacting the optically active amine I in the presence of hydrogen and a hydrogenation or dehydrogenation catalyst at elevated temperature, wherein the catalyst comprises the active components copper and zinc oxide and a support material.

    Abstract translation: 其中R1和R2不同且R1,R2,R3是烷基,环烷基,芳基烷基,芳基,杂芳基和杂环基的式I的光活性胺,R 3也可以是氢(H),其中基团能够带有取代基 选自由烷基,环烷基,烷氧基,芳氧基,氨基,烷基氨基和二烷基氨基组成的组,通过使光学活性胺I在氢气和氢化或脱氢催化剂的存在下在升高的温度下反应进行外消旋化,其中催化剂包含活性 组分铜和氧化锌和支撑材料。

    Alpha-methylstyrene dimer derivatives
    89.
    发明授权
    Alpha-methylstyrene dimer derivatives 失效
    α-甲基苯乙烯二聚体衍生物

    公开(公告)号:US06388153B2

    公开(公告)日:2002-05-14

    申请号:US09851549

    申请日:2001-05-09

    Abstract: The present invention relates to a method of making alpha-methylstyrene dimers by combining a cobalt catalyst, a free-radical initiator and an alpha-methylstyrene monomer, in an inert atmosphere, to form a mixture. The mixture is heated to a temperature in the range of 65° C. to 140° C. to form alpha methyl styrene dimers. The present invention also relates to the products produced by this inventive method.

    Abstract translation: 本发明涉及通过在惰性气氛中组合钴催化剂,自由基引发剂和α-甲基苯乙烯单体来制备α-甲基苯乙烯二聚体以形成混合物的方法。 将混合物加热至65℃至140℃的温度,以形成α-甲基苯乙烯二聚体。 本发明还涉及通过本发明方法生产的产品。

    Stereospecific isomerisation of allylamines with the aid of immobilized phosphorated chiral ligands
    90.
    发明授权
    Stereospecific isomerisation of allylamines with the aid of immobilized phosphorated chiral ligands 失效
    借助于固定化的磷酸化手性配体,烯丙胺的立体特异性异构化

    公开(公告)号:US06350910B1

    公开(公告)日:2002-02-26

    申请号:US09588687

    申请日:2000-06-07

    Abstract: The present invention describes a method for stereospecific isomerisation of prochiral allylamines into enamines and chiral imines, by using catalysts of Rh, Ir and Ru having phosphine chiral ligands immobilised on a solid material. The immobilised ligands are derivatives of phosphines of the type bis(diphenylphosphino)biaryl such as, for example, the phosphine known by the name BINAP. The method is particularly suitable for the production of optically active citronellal which may be obtained in optical purities above 95%.

    Abstract translation: 本发明描述了通过使用固定在固体材料上的具有膦手性配体的Rh,Ir和Ru的催化剂,将前手性烯丙胺立体特异性异构化成烯胺和手性亚胺的方法。 固定化的配体是双(二苯基膦基)联芳基类型的膦的衍生物,例如已知的名称为BINAP的膦。 该方法特别适用于光学纯度高于95%的光学活性香茅醛的制备。

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