Preparation of triazoles by organometallic addition to ketones and intermediates therefor
    7.
    发明授权
    Preparation of triazoles by organometallic addition to ketones and intermediates therefor 失效
    通过有机金属加成酮和其中间体制备三唑

    公开(公告)号:US06586594B1

    公开(公告)日:2003-07-01

    申请号:US09011346

    申请日:1998-02-04

    IPC分类号: C07D40310

    摘要: A process for the preparation of a compound of the formula: or an acid addition or base salt thereof, wherein R is phenyl optionally substituted by 1 to 3 substituents each independently selected from halo and trifluoromethyl; R1 is C1-C6 alkyl; and “Het” is pyrimidinyl optionally substituted by 1 to 3 substituents each independently selected from C1-C4 alkyl, C1-C4 alkoxy, halo, oxo, benzyl and benzyloxy, comprising reacting a compound of the formula: with a compound of the formula wherein X is chloro, bromo or iodo, the reaction taking place in the presence of zinc; at least one of iodine or a Lewis acid; and an aprotic organic solvent: optionally further reacting the resulting compound with an acid or base to form the corresponding acid addition or base salt thereof.

    摘要翻译: 一种制备下式化合物或其酸加成盐或碱盐的方法,其中R为任选被1-3个各自独立地选自卤素和三氟甲基的取代基取代的苯基; R1是C1-C6烷基; 和“Het”是任选被1至3个独立地选自C 1 -C 4烷基,C 1 -C 4烷氧基,卤素,氧代,苄基和苄氧基的取代基取代的嘧啶基,包括使下式化合物与式 是氯,溴或碘,反应发生在锌的存在下; 碘或路易斯酸中的至少一种; 和非质子有机溶剂:任选地使所得化合物与酸或碱进一步反应以形成相应的酸加成盐或碱盐。

    Process and intermediates for the preparation of thienopyrrole derivatives
    9.
    发明申请
    Process and intermediates for the preparation of thienopyrrole derivatives 失效
    制备噻吩并吡咯衍生物的方法和中间体

    公开(公告)号:US20050272938A1

    公开(公告)日:2005-12-08

    申请号:US10528612

    申请日:2003-09-29

    摘要: Novel Process and Intermediates. A process for preparing a compound of formula (I) where R4 and R5 are as defined in the specification; and R6 is hydrogen or a protecting group, which process comprises cyclisation of a compound of formula (II) where R4 and R5 and R6 are as defined in relation to formula (I), and R7 is nitrogen protecting group, and removing the group R7, and thereafter if desired, removing any protecting group R6. Novel intermediates and the use of these in the formation of pharmaceutical compounds is also described and claimed.

    摘要翻译: 新工艺和中间体。 制备其中R 4和R 5的式(I)化合物的方法如说明书中所定义; 和R 6是氢或保护基,该方法包括式(II)化合物的环化,其中R 4和R 5和R 5和 R 6如关于式(I)所定义,R 7为氮保护基,除去基团R 7,和 此后如果需要,除去任何保护基团R 6。 还描述和要求保护新型中间体及其在药物化合物形成中的用途。

    Chemical composition and use thereof
    10.
    发明授权
    Chemical composition and use thereof 失效
    化学成分及其用途

    公开(公告)号:US4754080A

    公开(公告)日:1988-06-28

    申请号:US34747

    申请日:1987-04-06

    IPC分类号: C07B39/00 C07C37/62 C07C39/24

    CPC分类号: C07C37/62 C07B39/00

    摘要: This invention relates to novel compositions comprising a N-halodialkylamine as defined in the specification and an inorganic oxide. The compositions are useful as halogenating agents for phenolic compounds. The compositions have the advantage that they are milder halogenating agents than halogens or hydrogen halides.

    摘要翻译: 本发明涉及包含本说明书中定义的N-卤代二烷基胺和无机氧化物的新型组合物。 该组合物可用作酚类化合物的卤化剂。 组合物的优点在于它们比卤素或卤化氢更温和的卤化剂。