[131I]-5-碘-N-[2-(6,7-二甲氧基-3,4-二氢-1H-异喹啉-2-基)乙基]-2-甲氧基苯甲酰胺作为一种潜在肿瘤显像剂的合成、放射性合成及体外评价
Synthesis, radiosynthesis, and in vitro evaluation of [131I]-5-iodo-N-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinoline-2-yl)-ethyl]-2-methoxy-benzamide as a potential tumor imaging agent.
作者信息
Xu Yu Ping, Yang Min, Pan Dong Hui
机构信息
The Key Laboratory of Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Ministry of Health, 20 Qianrong Road, Wuxi 214063, China.
出版信息
Appl Radiat Isot. 2009 Apr;67(4):594-7. doi: 10.1016/j.apradiso.2008.12.010. Epub 2008 Dec 24.
This work reports the synthesis, radiolabeling and preliminary in vitro evaluation of [(131)I]-5-iodo-N-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinoline-2-yl)-ethyl]-2-methoxy-benzamide. The tributylstannylprecursor was synthesized with a yield of 38%. Radiolabeling was performed using an electrophilic iododestannylation. Tracer yield was 94%, radiochemical purity was >95%. The tracer showed high uptake in MCF-7 breast cancer cell line and therefore will be evaluated further.
本研究报告了[(131)I]-5-碘-N-[2-(6,7-二甲氧基-3,4-二氢-1H-异喹啉-2-基)乙基]-2-甲氧基苯甲酰胺的合成、放射性标记及初步体外评估。三丁基锡前体的合成产率为38%。采用亲电碘脱锡反应进行放射性标记。示踪剂产率为94%，放射化学纯度>95%。该示踪剂在MCF-7乳腺癌细胞系中摄取率高，因此将进一步评估。
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