NEW [~(11)C]PHOSGENE BASED SYNTHESIS OF [~(11)C]PYRIMIDINES FOR POSITRON EMISSION TOMOGRAPHY

摘要

Thymine, 5-FU, and uracil were successfully synthesized through a procedure involving a cyclocondensation of triphosgene with newly developed α-substituted β-aminoacrylamides intermediates (1a, X= Me; 1b,X=F; 1c,X= H). The radioligands [2-~(11)C]thymine and [2-~(11)C]5-fluorouracil were synthesized in high radiochemical yields in 16-17 minutes from the end of bombardment by applying the cyclocondensation method with [~(11)C]COCl2.