申请人:MALLINCKRODT LLC
公开号:US20150087838A1
公开(公告)日:2015-03-26
The invention generally provides processes for the preparation of radioiodinated 3-fluoropropyl-nor-β-CIT. In particular, the process uses an arylsilane intermediate, thus avoiding the use of hexamethylditin, and reducing the number of steps previously required for the preparation of radioiodinated 3-fluoropropyl-nor-β-CIT from anhydroecgonine methyl ester. The invention also relates to the alkylation of a nortropane to the corresponding N-(3-fluoropropyl) analogue using 3-fluoropropanal.
该发明通常提供了用于制备放射性碘化3-氟丙基-去-β-CIT的方法。具体而言,该过程使用芳基硅烷中间体,从而避免使用六甲基锡,减少以前从去水基甲基植物碱制备放射性碘化3-氟丙基-去-β-CIT所需的步骤数量。该发明还涉及利用3-氟丙醛对去幽梗烷烃进行烷基化,形成相应的N-(3-氟丙基)类似物。