A novel and efficient synthesis of [2-11C]5-fluorouracil for prognosis of cancer chemotherapy.
OBJECTIVE
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.


METHODS
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.


CONCLUSIONS
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.
Seki
Koh-ichi
K
Central Institute of Radio Isotope Science, Hokkaido University, Kita-ku, Sapporo, Japan. seki@ric.hokudai.ac.jp
Nishijima
Ken-ichi
K
Kuge
Yuji
Y
Tamaki
Nagara
N
Wiebe
Leonard I
LI
Ohkura
Kazue
K
D000964:Antimetabolites, Antineoplastic / Q000737:chemistry* / Q000627:therapeutic use; D002250:Carbon Radioisotopes; D005472:Fluorouracil / Q000737:chemistry* / Q000627:therapeutic use; D009369:Neoplasms / Q000000981:diagnostic imaging* / Q000188:drug therapy; D049268:Positron-Emission Tomography; D011379:Prognosis; D019275:Radiopharmaceuticals / Q000138:chemical synthesis*
D000964:Antimetabolites, Antineoplastic; D002250:Carbon Radioisotopes; D019275:Radiopharmaceuticals; D005472:Fluorouracil