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为发展一种适合18F标记用于CAⅨ检测的特异性PET探针,该文以对氨基苯磺酰胺和三嗪为主要原料,用乙二醇、2-氟乙醇、对甲基苯磺酰氯对三嗪环进行适当修饰,合成了可能具有高亲和力和选择性的CAⅨ抑制剂4-[4-(2-氟乙氧基)-6-(2-羟基乙氧基)-1,3,5-三嗪-2-亚胺基]苯磺酰胺,用于前期生物学评价和探针放射化学合成的参比化合物,同时合成了用作18F标记的前体化合物4-(4,6-双[2-(4-甲基苯磺酰氧基)乙氧基]-1,3,5-三嗪-2-亚胺基)苯磺酰胺,这两个化合物的收率分别为27.6%和13.1%,可满足下一步放射化学标记的需要。上述工作为进一步发展CAⅨ特异性PET探针建立了基础。
In order to develop a specific PET probe suitable for 18F labeling for CAIX detection, this paper uses p-aminobenzenesulfonamide and triazine as the main raw materials, with ethylene glycol, 2-fluoroethanol, p-toluenesulfonyl chloride The triazine ring is suitably modified to synthesize the 4- [4- (2- fluoroethoxy) -6- (2-hydroxyethoxy) -1,3,5 -triazine-2-imino] benzenesulfonamide, a reference compound for use in the preliminary biological evaluation and probe radiochemical synthesis, was synthesized simultaneously as a 18F-labeled precursor compound 4- (4,6-bis [2- (4-methylbenzenesulfonyloxy) ethoxy] -1,3,5-triazine-2-imino) benzenesulfonamide, the yield of these two compounds was 27.6% and 13.1%, to meet the needs of the next step of radiochemical labeling. The above work has laid the foundation for the further development of CAIX-specific PET probes.