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| 1-[~(18)F]氟代乙基-L-色氨酸的半自动化合成 | |
| 引用本文： | 孙婷,王世真,唐刚华,李兆陇.1-[~(18)F]氟代乙基-L-色氨酸的半自动化合成[J].同位素,2010,23(2):86-92. |
| 作者姓名： | 孙婷 王世真 唐刚华 李兆陇 |
| 作者单位： | 1. 中国医学科学院,北京协和医学院,北京协和医院,核医学科,北京,100730 2. 中山大学附属第一医院,核医学科,广东,广州,510080 3. 清华大学,化学系,北京,100084 |
| 基金项目： | 国家自然科学基金项目，霍英东肺癌专项研究基金资助项目 |
| 摘 要： | 设计并合成了一种新型氟标记氨基酸类似物1-18F]氟代乙基-L-色氨酸(1-18F]FETrp)。以色氨酸为原料,采用有机合成法经过七步反应,合成了标准品1-19F]FETrp;使用氟多功能模块,采用亲核取代法,将放射化学标记自动化。经过对1-19F]FETrp自动化合成条件的摸索,最后采用二锅法合成了1-18F]FE-Trp。1-18F]FETrp的放化产率为1.5%,合成时间50 min;由于放化产率过低,今后需改变条件或者寻找新的合成路线以提高产率,以期为临床区分炎症和肿瘤提供新的PET显像剂。 |
| 关 键 词： | 1-[18F]氟代乙基-L-色氨酸（1-[18F]FETrp） PET显像剂 半自动化合成 |
Semi-automated Synthesis of 1-[18F]fluoroethyl-L-tryptophan |
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| SUN Ting,WANG Shih-Chen,TANG Gang-hua,LI Zhao-long.Semi-automated Synthesis of 1-[18F]fluoroethyl-L-tryptophan[J].Isotopes,2010,23(2):86-92. | |
| Authors: | SUN Ting WANG Shih-Chen TANG Gang-hua LI Zhao-long |
| Affiliation: | 1. Department of Nuclear Medicine, PUMC Hospital， Peking Union Medical College & Chinese Academy of Medical Sciences, Beijing 100730, China; 2. Department of Nuclear Medicine, the Frist Aflliated Hospital, Sun Yai-Sen University, Guangzhou 510080, China; 3.Department of Chemistry, Tsinghua University, Beijing 100084, China |
| Abstract: | A novel ~（18）F]fluoro amnio acid analogue 1-~（18）F]fluoroethyl-L-tryptophan（1-~（18）F]FETrp） was designed and synthesized.The cold standard 1-~（19）F]FETrp was synthesized by seven-step reactions,starting from tryptophan.Then fluoro-multifunctional chemistry process control unit（CPCU） was used to synthesize 1-~（19）F]FETrp by nucleophilic fluorination.1-~（18）F]FETrp was synthesized in a two-step semi-automated procedure.The no decay corrected radiochemica1 yield of 1-~（18）F]FETrp was 1.5% within 50 min total reaction time.Further experimental work is needed to improve the radiochemical yield,with the hope of attaining a satisfacting new PET imaging agent for differentiating the tumors and inflammation. |
| Keywords: | 1-[~（18）F]fluoroethyl-L-tryptophan（1-[~（18）F]FETrp） PET imaging agent semi-automated synthesis |
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