中文摘要：

以2-氨基-2-脱氧-D-葡萄糖为原料，通过微波加热法合成得到可用于核素标记的葡萄糖胺-1，4，7，10-四氮杂环十二烷-1，4，7，10-四乙酸（DOTA）前体化合物．产物通过IR，^1HNMR，HPLC-MS，ESI-HRMS表征．通过标记条件的优化设计，在微波作用下，与新型正电子显像核素Ga-68进行放射性标记，高产率得到68Ga—DOTA—DG．而后对该标记化合物进行了K-562，Hela，A431等肿瘤细胞摄取实验，测定了对肿瘤的特异性．68Ga—DOTA—DG的合成，拓宽了以18F-FDG为首的肿瘤代谢类显像剂的新应用，为PET（Positronemissiontomography）显像肿瘤代谢情况提供了一种新的途径．

英文摘要：

Starting from D-glucosamine （DG）, the precursor compound 2-（4-isothiocyanatobenzyl）- 1,4,7,10-tetraazacyclo-dodecane- 1,4,7,10-tetraacetic acid-D-glucose （DG-DOTA） was synthesized for potential radioactive imaging agents. Its structure was characterized by infrared, 1H NMR, LC-MS and ESI-HRMS. 6SGa is a generator-produced nuclide and does not require cyclotron on site. By careful selection of radiolabeling conditions, 68Ga-DOTA-DG was synthesized in short time and high yield by microwave synthesis system. Then, its binding affinity was tested by K-562, Hela and A431 tumor cell lines. The synthesis and evaluation of 68Ga-labeled DOTA-DG, not only provides a useful assessment of the stage of can- cer by imaging tumor metabolites compared with 1SF-FDG, but also develops a PET imaging agent.