[^(18)F]标记表皮生长因子受体抑制剂显像剂全自动合成方法

One-Pot Automatic Production of ^(18)F-labelled Tyrosine Kinase Inhibitor of Epidermal Growth Factor Receptor

目的:[18F]标记表皮生长因子受体酪氨酸激酶抑制剂(EGFR-TKI)正电子显像剂在指导肿瘤分子靶向治疗中具有非常重要的作用。本文目的是找到一种全自动、适合日常使用的[18F]标记EGFR-TKI正电子显像剂的全自动合成方法。方法:采用一步法合成[18F]EGFR-TKI PET显像剂。首先合成4-[18F]氟苯胺基,然后合成4-[18F]氟苯胺基-6,7-二甲氧基喹唑啉。结果:整个合成过程大约60分钟,产率25%-35%(未校正),放化纯度>95%。结论:本文建立了一种适合临床日常应用的[18F]EGFR-TKI PET显像剂的全自动合成方法。该方法对于进一步开发新型[18F]标记的表皮生长因子受体抑制剂PET显像具有重要价值。

ABSTRACT Objective： [^18F]-labelled tyrosine kinase inhibitor of epidermal growth factor receptor is often used for guidance on treatment of EGFR overexpressed cancer. Our objective is to develop a fully automatic method of routine production of [^18F]-labelled EGFR-TKI. Methods： A new one-pot method is used. The first step is synthesis of 4- [^18F] fluoroaniline, then 4- [^18F] fluorine based 6, 7- dimethoxy-anilinoquinazoline. Results： The total radiosynthesis time is 70 minutes after EOB. The radiochemical yield is 25%-35% （decay uncorrected）, and the radiochemical purity is more than 95%. Conclusion： The one-pot automatic synthesis of [^18F] labelled tyrosine kinase inhibitor of epidermal growth factor receptor is promising for routine use. Key words： [^18F]; EGFR-TKI; PET; Automatic synthesis