Efficient microscale synthesis of [18F]-2-fluoro-2-deoxy-d-glucose

• [18F]fluorination efficiency can be enhanced by flexible aliphatic tertiary alcohols.
• [18F]FDG was synthesized from mannose triflate on a micro-scale level with a higher radiochemical yield within shorter time.
• Radiosynthesis of [18F]FDG was influenced by ratio of tertiary alcohols and DMSO.
• The concentrations of mannose triflate and bases influence on the microscale substitution reaction yield.

Microscale radiosynthesis of [18F]FDG using a miniaturized device has been reported as a promising tool for positron emission tomography. However, small scale [18F]FDG radiosynthesis on micro fluidic devices need to be studied further to evaluate its usefulness. This paper analyzes several micro-scale reactions of [18F]FDG with various reaction conditions to achieve a higher radiochemical yield of [18F]FDG. Synthesis of [18F]FDG was carried out using mannose triflate on a microchip, and the crude product was purified via cartridge purification. The reaction conditions were optimized by examining several factors including reaction solvents, bases and their concentrations, that influence microscale radio synthesis of [18F]FDG. Based on the investigation of several variables and their effects on the radio-synthetic reaction, [18F]FDG was successfully synthesized on a micro-scale level with a radiochemical yield of 71% and within shorter time frame than that of the traditional method. Moreover, purity of the product was greater than 99%. These results show that the new guideline provides a more efficient and effective method of microscale [18F]FDG radiosynthesis.

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