Purpose: In order to facilitate the use of the PET-based Strauss test for 5-FU sensitivity, a rapid and facile synthesis of [2-11C]5-fluorouracil ([2-11C]5-FU), based on = [11C]phosgene ([11C]COCl2), is reported.
Method: The key intermediate (E)-beta- benzoylamino-Alpha-fluoroacrylamide (1) and [11C]phosgene was submitted to cyclocondensation to give [2-11C]5-fluorouracil.
Results: [2-11C]5-Fluorouracil was synthesized in 17 min with high (25%) radiochemical yield.
Conclusion: The present study provides a rapid, simple, and efficient synthesis of [2-11C]5-FU, that would serve as a useful prognostic PET tracer for 5-FU chemotherapy.