Novel probes for imaging amyloid-β: F-18 and C-11 labeling of 2-(4-aminostyryl)benzoxazole derivatives

✍ Scribed by Hiroshi Shimadzu; Takahiro Suemoto; Masako Suzuki; Tsuyoshi Shiomitsu; Nobuyuki Okamura; Yukitsuka Kudo; Tohru Sawada

• Publisher: John Wiley and Sons
• Year: 2004
• Tongue: French
• Weight: 149 KB
• Volume: 47
• Category: Article
• ISSN: 0022-2135
• DOI: 10.1002/jlcr.811

✦ Synopsis

Abstract

2‐(4‐Methylaminostyryl)‐6‐(2‐[^18^F]fluoroethoxy)benzoxazole ([^18^F]BF‐168) was prepared and found to be a potential probe for imaging amyloid‐β. The precursor, a 6‐(2‐tosyloxyethoxy)benzoxazole derivative, was fluorinated with [^18^F]KF and Kryptofix 222 in acetonitrile, and the crude product purified by semi‐preparative HPLC to give [^18^F]BF‐168. The radiochemical purity was >95% and the maximum specific activity was 106 TBq/mmol at the end of synthesis. The synthesis time was 110 min from the end of bombardment.

2‐(4‐[N‐methyl‐^11^C]methylaminostyryl)‐5‐fluorobenzoxazole ([^11^C]BF‐145) was also prepared from 2‐(4‐aminostyryl)‐5‐fluorobenzoxazole, [^11^C]MeI and 5 N NaOH in DMSO, and purified by semi‐preparative HPLC. The radiochemical purity was >95% and the specific activity was 40–70 TBq/mmol at the end of synthesis. The synthesis time was 45 min from the end of bombardment. Copyright © 2004 John Wiley & Sons, Ltd.