Automated synthesis of PET radiotracers by copper-mediated F-18-fluorination of organoborons: Importance of the order of addition and competing protodeborylation

作者：Mossine Andrew V; Brooks Allen F; Bernard Gauthier Vadim; Bailey Justin J; Ichiishi Naoko; Schirrmacher Ralf^*; Sanford Melanie S^*; Scott Peter J H^*

来源：Journal of Labelled Compounds and Radiopharmaceuticals, 2018, 61(3): 228-236.

DOI：10.1002/jlcr.3583

• automated radiosynthesis
• automation
• F18
• fluorine-18
• late-stage fluorination
• PET chemistry
• radiochemistry

In this paper, we describe the use of Cu-mediated [F-18]fluorodeboronation for the automated production of positron emission tomography radiotracers suitable for clinical use. Two recurrent issues with the method, low radiochemical conversion on automation and protoarene byproduct purification issues, have been successfully addressed. The new method was utilized to produce sterile injectable doses of [F-18]-(+/-)-IPMICF17, a positron emission tomography radiotracer for tropomyosin receptor kinase B/C, using an automated synthesis module. The product was isolated in 1.9 +/- 0.1% isolated radiochemical yield, excellent radiochemical purity (>99%), and high specific activity (5294 +/- 1227Ci/mmol). Quality control testing confirmed that doses were suitable for clinical use.

• 出版日期2018-3