achieved from beta-chloroaldehyde 3 in 4 and 5 steps, respectively, with an overall yield of 25-28%. [(18)F]Fluoroethylamine was prepared by heating N-[2-(toluene-4-sulfonyloxy)ethyl]phthalimide with [(18)F]fluoride ion in acetonitrile. [(18)F]1 was obtained by slow distillation under argon of [(18) F]FCH2CH2NH2 into amine 10 that was pre-treated with triphosgene at 0-5 °C. The total time required for
哺乳动物
雷帕霉素靶蛋白 (mTOR) 在细胞增殖的许多方面起着关键作用,最近的证据表明,改变的 mTOR 信号通路在衰老、肿瘤进展、神经精神疾病和重度抑郁症的发病机制中起着核心作用。mTOR 特异性 PET 示踪剂的可用性将有助于监测对临床开发中的
mTOR 抑制剂治疗的早期反应。为此,我们开发了 [(18)F]1-(4-(4-(8-oxa-3-azabicyclo[3.2.1]octan-3-yl)-1-(2,2,2) -三
氟乙基)-1H-
吡唑并[3,4-d]
嘧啶-6-基)苯基)-3-(2-
氟乙基)
脲[(18)F]
ATPFU([(18)F]1)作为mTOR PET
配体。参考文献 1 和放射性标记前体的合成,4-(4-8-oxa-3-azabicyclo[3.2.1]-octan-3yl)-1-(2,2,2-trifluoroethyl)-1H-pyrazolo[3 ,4-d]
嘧啶-6基)
苯胺(10),分别通过