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    • 6. 发明申请
    • PROCESS FOR TETRAAZACYCLOALKANE PREPARATION
    • 四氯化碳制剂的制备方法
    • WO1996028432A1
    • 1996-09-19
    • PCT/GB1996000462
    • 1996-03-01
    • NYCOMED IMAGING A/SCOCKBAIN, JulianSANDNES, Rolf, WiggoVASILEVSKIS, JanisUNDHEIM, KjellGACEK, Michel
    • NYCOMED IMAGING A/SCOCKBAIN, Julian
    • C07D257/02
    • C07D257/02
    • The present invention provides a synthetic route for tetraazacycloalkane preparation which facilitates heteropoly-N-alkylation of the macrocyclic product, and is thereby beneficial for the production of chelating agents and chelates useful in diagnostic imaging. The process involves (i) reacting a tetraazaalkane with a bridging agent to couple for amine nitrogens of said tetraazaalkane to a bridging moiety to yield a fused tricyclic intermediate, (ii) reacting said intermediate to introduce an alkylene bridge between the secondary amine nitrogens in the outer rings of the fused tricyclic intermediate, optionally be decoupling an alkanediylidene bridging moiety from the tertiary amine nitrogens at the ring fusion sites of the fused tricyclic intermediate, and (iii) where necessary, decoupling said bridging moiety to yield a macrocyclic tetraazacycloalkane.
    • 本发明提供了促进大环杂多杂-N-烷基化的四氮杂环烷烃制备的合成路线,从而有利于制备可用于诊断成像的螯合剂和螯合物。 该方法包括(i)使四氮杂链烷烃与桥连剂反应以将所述四氮杂烷的胺氮偶联至桥连部分以产生稠合的三环中间体,(ii)使所述中间体在仲胺氮中引入亚烷基桥, 稠合三环中间体的外环任选地在稠合三环中间体的环融合位点处将烷二亚烷基桥连部分与叔胺氮键分离,和(iii)必要时将所述桥连部分解偶联以产生大环四氮杂环烷烃。