Palladium catalyzed ring closure of triazolyltryptamine
    4.
    发明授权
    Palladium catalyzed ring closure of triazolyltryptamine 失效
    钯催化三唑基色胺的闭环

    公开(公告)号:US5567824A

    公开(公告)日:1996-10-22

    申请号:US248288

    申请日:1994-05-24

    摘要: A new process is described for the synthesis of the triazolyl tryptamine: ##STR1## and related compounds. The process involves a palladium-catalyzed ring closure between a substituted ortho-iodoaniline and a protected 1-alkynol. The process is carded out at high temperature, e.g. 100.degree. C., in a dry inert solvent, e.g., DMF and in the presence of a proton acceptor, e.g., Na.sub.2 CO.sub.3 or a trialkylamine. The triazolyl tryptamine, as well as acid addition salts thereof, is a 5 HT.sub.1 D receptor agonist having anti-migraine properties.

    摘要翻译: 描述了三唑基色胺的合成的新方法:< IMAGE>和相关化合物。 该方法涉及取代的邻碘苯胺和被保护的1-炔醇之间的钯催化的闭环。 该过程在高温下梳理,例如 在干惰性溶剂如DMF中并在质子受体例如Na 2 CO 3或三烷基胺存在下进行。 三唑基色胺及其酸加成盐是具有抗偏头痛性质的5 HT1D受体激动剂。

    Process for the preparation of imidazolutidine
    6.
    发明授权
    Process for the preparation of imidazolutidine 失效
    咪唑啉胺的制备方法

    公开(公告)号:US5424432A

    公开(公告)日:1995-06-13

    申请号:US249425

    申请日:1994-05-26

    IPC分类号: C07D471/04

    CPC分类号: C07D471/04

    摘要: This invention relates to a method for the preparation of a compound of formula I: ##STR1## a key intermediate in the synthesis of a series of Angiotensin II receptor antagonists. The invention also relates to a selective reagent for conducting the Hofmann rearrangement, particularly in the formation of a pyridinoimidazolone, which is a percursor to the formation of an imidazopyfidine of formula I. This invention also relates to a method for the preparation of imidazolutidine, a key intermediate in the synthesis of 3-(2'-(N-benzoyl)sulfonamidobiphen-4-yl)-methyl-5,7 -dimethyl-2-ethyl-3H-imidazo[4,5-b]pyridine, using pyridinoimidazolone, an unreactive urea.

    摘要翻译: 本发明涉及一种制备式I化合物的方法:作为合成一系列血管紧张素II受体拮抗剂的关键中间体。 本发明还涉及用于进行霍夫曼重排的选择性试剂,特别是形成吡啶并咪唑酮,该吡啶并咪唑酮是形成式I咪唑吡啶的方法。本发明还涉及制备咪唑烷丁的方法, 使用吡啶并咪唑啉酮合成3-(2' - (N-苯甲酰基)磺酰胺联苯-4-基) - 甲基-5,7-二甲基-2-乙基-3H-咪唑并[4,5-b]吡啶的关键中间体 ,非反应性尿素。