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1-[^(18)F]氟代乙基-L-色氨酸的半自动化合成 被引量：1

Semi-automated Synthesis of 1-[^(18)F]fluoroethyl-L-tryptophan
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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。 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.
作者 孙婷 王世真 唐刚华 李兆陇
机构地区 中国医学科学院北京协和医学院北京协和医院核医学科 中山大学附属第一医院核医学科 清华大学化学系
出处 《同位素》 CAS 2010年第2期86-92,共7页 Journal of Isotopes
基金 国家自然科学基金项目(30600154) 霍英东肺癌专项研究基金资助项目(2006207)
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 1-[^（18）F]fluoroethyl-L-tryptophan（1-[^（18）F]FETrp） PET imaging agent semi-automated synthesis
分类号 TQ463.7 [化学工程—制药化工] R817.9 [医药卫生—影像医学与核医学]
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参考文献16

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