Synthesis of radio-iodinated melatonergic agents

✍ Scribed by Douglas D. Dischino; Ronald J. Mattson; Marc D. Ogan; Michael F. Parker; Joseph P. Yevich

• Book ID: 102372306
• Publisher: John Wiley and Sons
• Year: 2002
• Tongue: French
• Weight: 103 KB
• Volume: 45
• Category: Article
• ISSN: 0022-2135
• DOI: 10.1002/jlcr.618

✦ Synopsis

Abstract

The synthesis of two ^125^I‐labeled trisubstituted aromatic melatonergic agents is reported. N‐[[2‐[^125^I]iodo‐5‐methoxyphenyl)‐1R, 2R‐cyclopropyl]methyl] butanamide was prepared from the corresponding thallium salt and Na ^125^I in radiochemical yields of 13–45% (n = 3). High performance liquid chromatography separation of the two resulting radioiodinated isomers (8:2) from each other and the parent compound required the use of two different columns run in series. Synthesis of N‐[[2‐[^125^I]iodo‐5‐fluorophenyl)‐1R, 2R‐cyclopropyl]methyl] butanamide was prepared from the corresponding trimethylstannane precursor in radiochemical yields consistently in the range of 60–65% (n = 6). Copyright © 2002 John Wiley & Sons, Ltd.