A rapid microfluidic synthesis of [F-18]fluoroarenes from nitroarenes

作者：Moore Thomas M; Akula Murthy R; Collier Lee; Kabalka George W^*

来源：Applied Radiation and Isotopes, 2013, 71(1): 47-50.

DOI：10.1016/j.apradiso.2012.09.013

• Radiofluorination
• Fluordenitration
• Aromatic Fluorinatio
• Microfluidics
• Automation

Microfluidic radiofluorodenitrations have been successfully performed using a commercially available microfluidic synthesis system. Reactions of nitroarenes with para-substituted electron withdrawing groups provide incorporation yields ranging from 43 to 97%. Ortho- and meta-substituted nitroarenes provided incorporation yields up to 35%. The reactions were conducted using dry, no-carrier-added [F-18]-fluoride and K2CO3/K-222 dissolved in N,N-dimethylformamide or dimethyl sulfoxide with total synthesis times of less than five min. The methodology developed in these studies can be applied to the synthesis of a variety of fluorine-18 labeled radiotracers and radiolabeled prosthetic groups from nitroarene precursors.

• 出版日期2013-1