Radiosynthesis of 13N-labeled thalidomide using no-carrier-added [13N]NH3

✍ Scribed by Katsushi Kumata; Makoto Takei; Masanao Ogawa; Joji Yui; Akiko Hatori; Kazutoshi Suzuki; Ming-Rong Zhang

• Publisher: John Wiley and Sons
• Year: 2010
• Tongue: French
• Weight: 216 KB
• Volume: 53
• Category: Article
• ISSN: 0022-2135
• DOI: 10.1002/jlcr.1699

✦ Synopsis

Abstract

Recent studies revealed that thalidomide (1) has unique and broad pharmacological effects on multi‐targets although the application of 1 in therapy is still controversial. In this study, we synthesized nitrogen‐13‐labeled thalidomide ([^13^N]1) as a potential positron emission tomography (PET) probe using no‐carrier‐added [^13^N]NH~3~ as a labeling agent. By use of an automated system, [^13^N]1 was prepared by reacting N‐phthaloylglutamic anhydride (2) with [^13^N]NH~3~, following by cyclization with carbonyldiimidazole in a radiochemical yield of 56±12% (based on [^11^N]NH~3~, corrected for decay) and specific activity of 49±24 GBq/µmol at the end of synthesis (EOS). At EOS, 570–780 MBq (n=7) of [^13^N]1 was obtained at a beam current of 15 µA after 15 min proton bombardment with a synthesis time of 14 min from the end of bombardment. Using a small animal PET scanner, preliminary biodistribution of [^13^N]1 in mice was examined. Copyright © 2010 John Wiley & Sons, Ltd.