Rapid 18F-radiolabeling of peptides from [18F]fluoride using a single microfluidics device

Abstract

To date the majority of ¹⁸F-peptide radiolabeling approaches are multi-step, low yielding and time-consuming processes. Given the short half-life of ¹⁸F (109.8 min), it is critical that methods are developed to increase the efficiency of this process with simpler, higher yielding and faster reactions that can be rapidly translated into clinical use. Here, we demonstrate the first microfluidic synthesis of the [¹⁸F]F-Py-TFP prosthetic group with radiochemical yields of up to 97% and a synthesis time of 3 min. In addition, we utilized a single microfluidics device to prepare the [¹⁸F]F-Py-YGGFL peptide using [¹⁸F]F-Py-TFP, from [¹⁸F]fluoride in a two-step, fully automated approach. The model peptide NH₂-YGGFL was radiolabeled with [¹⁸F]F-Py-TFP in up to 28% overall radiochemical yield within 8 minutes starting from anhydrous [¹⁸F]fluoride.