发明名称 Catalytic Radiofluorination
摘要 One aspect of the present invention relates to a method of preparing radiofluorinated substituted alkyl, cycloalkyl, aryl, and alkenyl compounds. In a preferred embodiment, potassium fluoride-18 is used. Another aspect of the invention relates to piperazine compounds containing fluorine-18 that are useful as imaging agents. In certain embodiments, the piperazine compounds contain a quaternary amine. Another aspect of the invention relates to arylphosphonium compounds containing fluorine-18 that are useful as imaging agents. In certain embodiments, the phosphonium compound is a tetraaryl phosphonium salt. Another aspect of the present invention relates to a method of obtaining a positron emission image of a mammal, comprising the steps of administering to a mammal a compound of the invention, and acquiring a positron emission spectrum of the mammal.
申请公布号 US2015283273(A1) 申请公布日期 2015.10.08
申请号 US201514695176 申请日期 2015.04.24
申请人 The General Hospital Corporation 发明人 Elmaleh David R.;Fischman Alan J.;Shoup Timothy M.
分类号 A61K51/04;C07F9/54;C07D295/073 主分类号 A61K51/04
代理机构 代理人
主权项 1. A method according to Scheme 3:wherein A is aryl, heteroaryl, aralkyl, alkenyl or has the formula a or b: wherein R1 represents independently for each occurrence alkyl, cycloalkyl, aryl, or heteroaryl; R2 represents alkylene, cycloalkylene, arylene, or heteroarylene; R3 represents independently for each occurrence H, alkyl, or halogen; R4 represents independently for each occurrence H, alkyl, halogen, hydroxyl, amino, aminoalkyl, or alkoxyl; R5 is H, alkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, aralkyl, heteroaralkyl, acyl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, or —CO2H; and Z is halide, nitrate, acetate, benzoate, or sulfonate; X is sulfonate, nitro, acetate, halogen, sulfate, or phosphate; M is an alkali metal, transition metal, or ammonium; Y is fluoride or iodide; A is non-covalently bound to a transition metal cation; and the method is practiced under substantially anhydrous conditions.
地址 Boston MA US