16α-[18F]-fluoroestradiol ([18F]FES) is known as a clinically important tracer in nuclear medicine as an estrogen receptor (ER) ligand for investigating primary and metastatic breast cancers. Synthesizing [18F]FES is a two-step process associated with [18F]fluoride incorporation to the precursor (3-methoxymethyl 16β, 17β-epiestriol-O-cyclic sulfone, MMSE) and subsequent hydrolysis of the [18F]fluorinated intermediate with 2N HCl. The impact of microwave heating (MW) on both fluorination and hydrolysis reactions was investigated. The duration and temperatures of the fluorination reaction were varied for both MW and conventional heating (CH) methods. Chemical and radiochemical purities and radiochemical yields were investigated for CH and compared to microwave-assisted radiosyntheses. Quality control tests of microwave-assisted [18F]FES were performed following United States Pharmacopeia (USP) procedures for clinical-grade positron emission tomography (PET) pharmaceuticals. The results demonstrate that microwaving not only improves the 18F-fluoride incorporation (~ 55% improvement at 110 °C for 4 min) but also significantly reduces hydrolysis time (~ 7-fold reduction at 120 °C) in compare to CH under similar conditions. The overall isolated radiochemical yield of purified [18F]FES was significantly higher (~ 90% improvement) with MW, and side-products were notably fewer. Quality control test results demonstrated that [18F]FES produced by microwaving was suitable for human injection.
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