18F-AV45是首个FDA批准上市的阿兹海默症(AD)显像用PET药物,其异构体18F-YG也可能具有更好的性能。为促进18F-AV45的国产化及评价其异构体18F-YG在AD显像方面的性能,本工作合成了两者的标记前体化合物。具体方法为:以4-氨基苯乙烯为原料...18F-AV45是首个FDA批准上市的阿兹海默症(AD)显像用PET药物,其异构体18F-YG也可能具有更好的性能。为促进18F-AV45的国产化及评价其异构体18F-YG在AD显像方面的性能,本工作合成了两者的标记前体化合物。具体方法为:以4-氨基苯乙烯为原料,经过碳酸叔丁基保护和碘甲烷甲基化,得到BOC保护的对甲胺基苯乙烯;该苯乙烯结构双键上的氢原子被TEG链修饰过的碘吡啶取代后,以对甲苯磺酸基保护TEG侧链羟基,得到目标产物AV105和YGQT,总产率分别为57%和66%。ESI-MS、1 H NMR验证结果显示,两种前体化合物结构正确。前体化合物AV105和YGQT的合成为进一步研究18F-AV45及其异构体18F-YG在AD显像方面的性能提供了基础。展开更多
The solution reaction mechanisms,composition,donor atoms,properties of coordinate link and stability of the complexes on the systems of adrenaline with Na^(3+),Gd^(3+)and Tm^(3+)have been studied by pH-potentiometric ...The solution reaction mechanisms,composition,donor atoms,properties of coordinate link and stability of the complexes on the systems of adrenaline with Na^(3+),Gd^(3+)and Tm^(3+)have been studied by pH-potentiometric titration and electronic spectroscopy.Adrenaline perturbs the f-f electronic transition of Nd^(3+)and Tm^(3+)so that the absorption spectra of their complexes are shifted toward longer wavelengths.The absorption spectra of the complexes formed by the three f-block element ions with adrenaline are shifted toward shorter wavelengths with the increase of PH in Δγ=350～650 nm展开更多
文摘18F-AV45是首个FDA批准上市的阿兹海默症(AD)显像用PET药物,其异构体18F-YG也可能具有更好的性能。为促进18F-AV45的国产化及评价其异构体18F-YG在AD显像方面的性能,本工作合成了两者的标记前体化合物。具体方法为:以4-氨基苯乙烯为原料,经过碳酸叔丁基保护和碘甲烷甲基化,得到BOC保护的对甲胺基苯乙烯;该苯乙烯结构双键上的氢原子被TEG链修饰过的碘吡啶取代后,以对甲苯磺酸基保护TEG侧链羟基,得到目标产物AV105和YGQT,总产率分别为57%和66%。ESI-MS、1 H NMR验证结果显示,两种前体化合物结构正确。前体化合物AV105和YGQT的合成为进一步研究18F-AV45及其异构体18F-YG在AD显像方面的性能提供了基础。
文摘The solution reaction mechanisms,composition,donor atoms,properties of coordinate link and stability of the complexes on the systems of adrenaline with Na^(3+),Gd^(3+)and Tm^(3+)have been studied by pH-potentiometric titration and electronic spectroscopy.Adrenaline perturbs the f-f electronic transition of Nd^(3+)and Tm^(3+)so that the absorption spectra of their complexes are shifted toward longer wavelengths.The absorption spectra of the complexes formed by the three f-block element ions with adrenaline are shifted toward shorter wavelengths with the increase of PH in Δγ=350～650 nm
