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

利用铜介导的有机硼化合物的 (18)F-氟化反应自动合成PET放射性示踪剂:加成顺序和竞争性质子脱硼反应的重要性

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Abstract

In this paper, we describe the use of Cu-mediated [(18) F]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 [(18) F]-(±)-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 ± 1227 Ci/mmol). Quality control testing confirmed that doses were suitable for clinical use.

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