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13 条记录 (耗时 0.014 秒)

    Process for the production of threo-4-alkoxy-5- (arylhydroxymethyl)-2(5H)-furanones
    4.
    发明授权
    Process for the production of threo-4-alkoxy-5- (arylhydroxymethyl)-2(5H)-furanones 失效
    生产甲基-4-烷氧基-5-（芳基甲基）-2（5H） - 呋喃酮的方法

    公开(公告)号：US5200531A

    公开(公告)日：1993-04-06

    申请号：US808761

    申请日：1991-12-17

    申请人： David Laffan

    发明人： David Laffan

    IPC分类号： A61K31/34 ,  A61K31/341 ,  A61P25/08 ,  B01J23/04 ,  C07B61/00 ,  C07D307/60

    CPC分类号： C07D307/60

    摘要： Threo-4-alkoxy-5-(arylhydroxymethyl)-2(5H)-furanones are obtained by condensation of 4-alkoxy-2(5H)-furanones with benzaldehydes in the presence of lithium hydroxide without contamination by the corresponding erythro stereoisomers. The condensation is preferably performed in aqueous acetonitrile and the product is precipitated from the alkaline reaction mixture by the addition of water. The products that can be produced according to the process of the invention are known pharmaceutical active ingredients with anticonvulsive or antiepileptic action.

    摘要翻译： 在氢氧化锂存在下，通过4-烷氧基-2（5H） - 呋喃酮与苯甲醛的缩合而得到4-（烷基羟基甲基）-2（5H） - 呋喃酮，而不会被相应的红立体异构体污染。 缩合优选在乙腈水溶液中进行，并通过加入水从碱性反应混合物中沉淀产物。 可以根据本发明的方法生产的产品是具有抗惊厥或抗癫痫作用的已知药物活性成分。

    Process for the preparation of substituted pentaalkylchromenes
    7.
    发明授权
    Process for the preparation of substituted pentaalkylchromenes 失效
    制备取代五烷基色烯的方法

    公开(公告)号：US5364946A

    公开(公告)日：1994-11-15

    申请号：US977157

    申请日：1992-11-16

    申请人： David Laffan

    发明人： David Laffan

    IPC分类号： C07B61/00 ,  C07C46/08 ,  C07C50/24 ,  C07D311/58 ,  C07D311/70 ,  C07D311/04

    CPC分类号： C07D311/70 ,  C07C46/08 ,  C07C50/24 ,  C07D311/58

    摘要： A novel process the preparation of pentaalkylchromenes of the general formula: ##STR1## wherein R denotes a lower alkyl group having 1 to 4 C atoms and R.sub.1 denotes a phenyl group which is unsubstituted or substituted by a lower alkyl group having 1 to 4 C atoms, by halogen or by a nitro group, or an alkanoyl group having 1 to 4 C atoms. In the process, a trialkylhydroquinone is reacted with a halogenated butenol to give a substituted tetraalkyhydroquinone, which is oxidized. Then the halogen atom is substituted with a suitable nucleophile and the compound is finally cyclized to give the final product. The pentaalkylchromenes are suitable intermediates for the preparation of hypolipidaemic pharmaceuticals.

    摘要翻译： 一种新方法制备通式如下的五烷基色烯：其中R表示具有1至4个C原子的低级烷基，R 1表示未被取代或被具有1至4个碳原子的低级烷基取代的苯基 原子，卤素或硝基，或具有1〜4个C原子的烷酰基。 在此过程中，使三烷基氢醌与卤代丁烯醇反应，得到被氧化的取代四烷基氢醌。 然后用合适的亲核试剂取代卤素原子，最终将化合物环化得到最终产物。 五烷基色烯是用于制备降血脂药物的合适的中间体。

    Process for the preparation of substituted pentaalkylchromenes
    8.
    发明授权
    Process for the preparation of substituted pentaalkylchromenes 失效
    制备取代五烷基色烯的方法

    公开(公告)号：US5304663A

    公开(公告)日：1994-04-19

    申请号：US120789

    申请日：1993-09-15

    申请人： David Laffan

    发明人： David Laffan

    IPC分类号： C07B61/00 ,  C07C46/08 ,  C07C50/24 ,  C07D311/58 ,  C07D311/70 ,  C07C50/06

    CPC分类号： C07D311/70 ,  C07C46/08 ,  C07C50/24 ,  C07D311/58

    摘要： A novel process for the preparation of pentaalkylchromenes of the general formula: ##STR1## wherein R denotes a lower alkyl group having 1 to 4 C atoms and R.sub.1 denotes a phenyl group which is unsubstituted or substituted by a lower alkyl group having 1 to 4 C atoms, by halogen or by a nitro group, or an alkanoyl group having 1 to 4 C atoms. In the process, a trialkylhydroquinone is reacted with a halogenated butenol to give a substituted tetraalkyhydroquinone, which is oxidized. Then the halogen atom is substituted with a suitable nucleophile and the compound is finally cyclized to give the final product. The pentaalkylchromenes are suitable intermediates for the preparation of hypolipidaemic pharmaceuticals.

    摘要翻译： 一种制备通式如下的五烷基色烯的新方法：其中R表示具有1至4个C原子的低级烷基，R 1表示未被取代或被具有1-4个碳原子的低级烷基取代的苯基 C原子，卤素或硝基，或具有1-4个C原子的烷酰基。 在此过程中，使三烷基氢醌与卤代丁烯醇反应，得到被氧化的取代四烷基氢醌。 然后用合适的亲核试剂取代卤素原子，最终将化合物环化得到最终产物。 五烷基色烯是用于制备降血脂药物的合适的中间体。

    Process and intermediates for the production of 7-substituted antiestrogens
    9.
    发明申请
    Process and intermediates for the production of 7-substituted antiestrogens 有权
    用于生产7-取代的抗雌激素的方法和中间体

    公开(公告)号：US20050101583A1

    公开(公告)日：2005-05-12

    申请号：US10398924

    申请日：2001-10-09

    申请人： Robert Stevenson ,  Fraser Kerr ,  Anthony Lane ,  Eve Brazier ,  Philip Hogan ,  David Laffan

    发明人： Robert Stevenson ,  Fraser Kerr ,  Anthony Lane ,  Eve Brazier ,  Philip Hogan ,  David Laffan

    IPC分类号： C07B61/00 ,  C07J31/00 ,  C07J41/00 ,  C07J75/00 ,  A61K31/56 ,  C07J1/00

    CPC分类号： C07J31/006 ,  C07J31/00 ,  Y02P20/55

    摘要： A process for preparing an intermediate compound of formula (II) where X is as defined in the specification, R1 is haloalkyl, alkyl, alkenyl, cycloalkyl, carboxyalkyl, alkoxycarbonylalkyl, aryl or arylalkyl; R2, R3, R4 and R5 are organic groups as defined in the specification, which process comprises aromatisation of a compound of formula (III) where R1, R2, R3, n, X and R5 are as defined in relation to formula (II) and R4′ is a group R4 or a precursor group thereof, and thereafter if necessary or desired, carrying out one or more of the following steps: (i) removing any hydroxy-protecting groups R; (ii) converting a precursor group R4′ to a group R4, or where R4′ is a group R4, converting it to a different such group. Compounds obtained are useful intermediates for example in the preparation of fulvestrant. Novel intermediates are also claimed.

    摘要翻译： 制备其中X如说明书中所定义的式（II）的中间体化合物的方法是卤代烷基，烷基，烯基，环烷基，羧基烷基，烷氧基羰基烷基，芳基或芳基烷基; R 2，R 3，R 4和R 5是说明书中定义的有机基团，该方法 包括式（III）化合物的芳构化，其中R 1，R 2，R 3，R 3，n，X和R 5 如式（II）所定义，并且R 4'是基团R 4或其前体基团，然后如果需要或需要， 进行一个或多个以下步骤：（i）除去任何羟基保护基团R; （ii）将前体基团R 4'转化成基团R 4，或其中R 4'是基团R 4 ，将其转换为不同的这样的组。 获得的化合物是例如制备氟维司群的有用的中间体。 还要求新的中间体。

    Catalysts containing zirconium oxide
    10.
    发明授权
    Catalysts containing zirconium oxide 失效
    含氧化锆的催化剂

    公开(公告)号：US6075145A

    公开(公告)日：2000-06-13

    申请号：US35839

    申请日：1998-03-06

    申请人： Josef Heveling ,  David Laffan ,  Alain Wellig

    发明人： Josef Heveling ,  David Laffan ,  Alain Wellig

    IPC分类号： C07D453/02 ,  B01J21/06 ,  B01J23/72 ,  B01J23/755 ,  B01J35/10 ,  C01G25/00 ,  C01G25/02 ,  C07C29/14 ,  C07C29/143 ,  C07C45/29

    CPC分类号： B01J23/755 ,  C07C29/14 ,  C07C29/143 ,  C07C45/29 ,  C07B2200/09

    摘要： Catalyst compositions based on amorphous partially dehydrated zirconium hydroxide which are doped with from 0.01 to 20 atom percent of copper and/or from 0.01 to 20 atom percent of nickel, in each case based on zirconium, and have a specific surface area by the BET method of at least 50 m.sup.2 /g. The catalyst compositions are suitable, in particular, as the catalyst in hydrogen transfer reactions, such as, the Meerwein-Ponndorf-Verley reduction or the Oppenauer oxidation. The preparation of 3-hydroxyquinuclidine of the formula: ##STR1## involves reaction of quinuclidin-3-one with a secondary alcohol in the presence of the amorphous partially dehydrated zirconium hydroxide.

    摘要翻译： 基于无定形部分脱氢的氢氧化锆的催化剂组合物，其掺杂有0.01至20原子％的铜和/或0.01至20原子％的镍，每种情况基于锆，并且通过BET法具有比表面积 至少50m2 / g。 催化剂组合物特别适合作为氢转移反应中的催化剂，例如Meerwein-Ponndorf-Verley还原剂或Oppenauer氧化剂。 制备下式的3-羟基奎宁环：包括在无定形部分脱水的氢氧化锆存在下，将奎宁环-3-酮与仲醇反应。