Synthesis and labeling of epidepride

作     者：YANG Min, PEI Zhu-Guo, HU Ming-Yang, WANG Bo-Cheng, ZHOU Xing-Qin (State Key Laboratory of Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063) 

出 版 物：《Nuclear Science and Techniques》 (核技术（英文）)

年 卷 期：2001年第12卷第2期

页      面：111-116页

核心收录：

学科分类：081704[工学-应用化学] 07[理学] 08[工学] 0817[工学-化学工程与技术] 070303[理学-有机化学] 0703[理学-化学] 

主　　题：放射医学 大脑神经 同位标记 

摘      要：S-(-)-N-[(1-ethyl-2-pyrrolidinyl)methyl]-5-iodo-2,3-dimethoxybenzamide (proposed generic name, epidepride) is a very potent dopamine D2 antagonist. It was synthesized by five steps from 3-methoxysalicylic acid. [131I]epidepride was obtained in 97.3% radiochemical yields from the corresponding 5-(tributyltin) derivative using hydrogen peroxide as the oxidant. The aryltin precursor was prepared from non-labelled epidepride by palladium-catalyzed stannylation using bis(tri-n-butyltin) in triethylamine. [131I]epidepride was stable under 4℃, and partition coefficient was 72.3 at pH 7.40. The biodistribution study in rats exihibited high localization in the striatum of the brain with the striatum/cerebellum ratio reaching 237/1 at 320 min postinjection. All these results suggest that [131I]epidepride may be used widely as a useful dopamine D2 receptor imaging agent for SPECT.