一种含氟原子和三嗪环的磺胺类化合物的合成  

Synthesis of Sulfonamide Compound with F Atom and Cyanuric Chloride Moieties

作　　者：武明星[1] 郭飞虎[2] 施玲丽[1] 包广粮[1] 郑明强[1] 韩彦江[1] 王妮[1] 周伟[1] 胡伟青[1] 沈华[1] 于俊峰[1] 沈玉梅[1] 尹端沚[1] 汪勇先[1] 张岚[1] 

机构地区：[1]中国科学院上海应用物理研究所放射性药物研究中心 [2]中国原子能科学研究院同位素研究所,北京102413

出　　处：《精细化工》2008年第10期945-947,955,共4页Fine Chemicals

基　　金：国家自然科学基金资助项目(20601028)~~

摘　　要：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 new carbonic anhydrase inhibitor （CAI） and further to synthesize a PET molecular imaging probe used for tumor hypoxia detecting, with 4-aminomethylbenzenesulfonamide hydrochloride and cyanuric chloride as major starting materials, and modified with glycol and 2- fluoroethanol, a potential CA Ⅸ inhibitor 4- { [ 4 - （ 2-fluoroethoxy ） 6- （ 2-hydroxyethoxy ） - 1,3,5 -triazin - 2-ylamino ] methyl l benzenesulfonamide was synthesized, which is expected to possess high affinity and excellent selectivity. This compound comprises sulfonamide which is the active segment, as well as F atom and triazine ring. So the compound is a potential CA inhibitor and will be used for the initial biological evaluation. It is also used as the reference compound for radiosynthesis of the labeled probe. The yield of this compounds is 18.5%. In our next as the reference compound for radiosynthesis of the work, it is used for initial biological evaluation and labeled probe.

关 键 词：碳酸酐酶 抑制剂 功能材料 

分 类 号：Q946.885.9[生物学—植物学]