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为开发一种新型碳酸酐酶抑制剂,并进一步合成一种检测肿瘤乏氧的PET分子影像探针,以4-氨基甲基苯磺酰胺盐酸盐、三嗪为主要起始原料,通过用2-氟乙醇、乙二醇对三嗪环加以修饰,合成了可能具有高亲和力和选择性的碳酸酐酶抑制剂4-{[4-(2-氟基乙氧基)-6-(2-羟基乙氧基)-1,3,5-三嗪-2-氨基]甲基}苯磺酰胺。该化合物含有碳酸酐酶抑制剂所含有的活性基团磺胺,同时含有氟原子和三嗪环,是个很有潜力的碳酸酐酶抑制剂,该化合物的总收率为18.5%,可用于下一步实验中的前期生物学评价和PET分子影像探针放射化学合成的参比化合物。
In order to develop a novel carbonic anhydrase inhibitor and further to synthesize a PET molecular imaging probe for detection of tumor hypoxia, 4-aminomethylbenzenesulfonamide hydrochloride and triazine are used as the main starting materials, 4 - {[4- (2-fluoroethoxy) -6- (2-fluoroethoxy) -6-fluoroquinolone was synthesized by the modification of triazine ring with 2-fluoroethanol and ethylene glycol. - hydroxyethoxy) -1,3,5-triazine-2-amino] methyl} benzenesulfonamide. This compound contains a sulfonic amine as an active group contained in a carbonic anhydrase inhibitor and contains both a fluorine atom and a triazine ring and is a very promising carbonic anhydrase inhibitor with an overall yield of 18.5% and can be used in the next step Experimental pre-biological evaluation and PET molecular imaging probe radiochemical synthesis of reference compounds.