STEREOSELECTIVE SYNTHESIS OF AMINO ACID ANALOGS FOR TUMOR IMAGING

摘要

The radiolabeled non-natural amino acid 1-amino-3- cyclobutane-1-carboxylicacid (ACBC) and its analogs are candidate tumor imaging agents useful forpositron emission tomography and single photon emission computed tomographydue to their selective affinity for tumor cells. The present inventionprovides methods for stereo-selective synthesis of syn-ACBC analogs. Thedisclosed synthetic strategy is reliable and efficient and can be used tosynthesize a gram quantity of various syn-isomers of the ACBC analogs,particularly, syn- [18F]-1-amino-3-fluorocyclobutane-1-carboxylic acid (FACBC)and syn- [123I]-1-amino-3-iodocyclobutane-1-carboxylic (IACBC) acid analogs.