微波加热法合成O-(2-~(18)F氟乙基)-L-酪氨酸

Radiosynthesis of O-(2-~(18)Ffluoroethyl)-L-tyrosine by Microwave Heating

摘要: O-(2-18F氟乙基)-L-酪氨酸(O-(2-18Ffluoroethyl)-L-Tyrosine,18F-FET)是最近研究的氨基酸类脑肿瘤PET显像剂。为了缩短合成时间,简化操作步骤,减少工作人员的辐射剂量,从反应组分、加热方法和反应模式等3个方面改进并优化18F-FET的“两步法”放射化学合成路线。实验选择L-酪氨酸和氢氧化钠溶液与DMSO作为反应组分,加热方式更换为微波法,采用简化的“一锅式”反应方式,总合成时间缩短至20 min,标记率大于95%。

Abstract: O-(2-~(18)Ffluoroethyl)-L-tyrosine, recently developed radiolabelled amino acids,is a very promising PET imaging agent for brain tumor diagnosis and holds hugely clinical potential.To(shorten) synthesis time,simplify operation process and lessen irradiation exposure to operator,radiosynthesis of O-(2-~(18)Ffluoroethyl)-L-tyrosine is adapted and optimized,according to three aspects of its two-step method, including reaction components,heating methods and reaction models.Introducing microwave heating,one-pot model and L-Tyr,NaOH-H_2O and DMSO as reactant,the total synthesis time is within 20min.