NEW ~(11)CPHOSGENE BASED SYNTHESIS OF ~(11)CPYRIMIDINES 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)Cthymine and 2-~(11)C5-fluorouracil were synthesized in high radiochemical yields in 16-17 minutes from the end of bombardment by applying the cyclocondensation method with ~(11)CCOCl2.