1-18F氟代乙基-L-色氨酸的半自动化合成

Semi-automated Synthesis of 1-18Ffluoroethyl-L-tryptophan

  • 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(1-18FFETrp)。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1-19FFETrp;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1-19FFETrp自动化合成条件的摸索,最后采用二锅法合成了1-18FFETrp。1-18FFETrp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 18Ffluoro amnio acid analogue 1-18Ffluoroethyl -L- tryptophan (1-18FFETrp) was designed and synthesized. The cold standard 1-19FFETrp was synthesized by sevenstep reactions, starting from tryptophan. Then fluoromultifunctional chemistry process control unit (CPCU) was used to synthesize 1-19FFETrp by nucleophilic fluorination. 1-18FFETrp was synthesized in a twostep semiautomated procedure. The no decay corrected radiochemica1 yield of 1-18FFETrp 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.

     

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