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1-[18F]氟代乙基-L-色氨酸的半自动化合成

Semi-automated Synthesis of 1-[18F]fluoroethyl-L-tryptophan

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【作者】 孙婷王世真唐刚华李兆陇

【Author】 SUN Ting1,WANG Shih-Chen1,TANG Gang-hua2,LI Zhao-long3(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)

【机构】 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

【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。

【Abstract】 A novel [18F]fluoro amnio acid analogue 1-[18F]fluoroethyl-L-tryptophan(1-[18F]FETrp) was designed and synthesized.The cold standard 1-[19F]FETrp was synthesized by seven-step reactions,starting from tryptophan.Then fluoro-multifunctional chemistry process control unit(CPCU) was used to synthesize 1-[19F]FETrp by nucleophilic fluorination.1-[18F]FETrp was synthesized in a two-step semi-automated procedure.The no decay corrected radiochemica1 yield of 1-[18F]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.

【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)
  • 【分类号】TQ463.7
  • 【被引频次】1
  • 【下载频次】107
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