Author:
Shirakami Yoshifumi,Watabe Tadashi,Obata Honoka,Kaneda Kazuko,Ooe Kazuhiro,Liu Yuwei,Teramoto Takahiro,Toyoshima Atsushi,Shinohara Atsushi,Shimosegawa Eku,Hatazawa Jun,Fukase Koichi
Abstract
AbstractAstatine-211 (211At)-labeled phenylalanine is expected to be a promising agent for targeted alpha-particle therapy for the treatment of patients with glioma. The existing reactions to prepare the labeled compound usually require organic solvents and metals that are toxic and hazardous to the environment. In this study, we developed a novel method wherein astatination was realized via the substitution of 211At for a dihydroxyboryl group coupled to phenylalanine. [211At]4-astato-L-phenylalanine was obtained as the carrier-free product in aqueous medium in high radiochemical yields (98.1 ± 1.9%, n = 5). The crude reaction mixture was purified by solid-phase extraction, and the radiochemical purity of the product was 99.3 ± 0.7% (n = 5). The high yield and purity were attributed to the formation of [211At]AtI and AtI2− as the reactive intermediates in the astatination reaction. The reaction did not require any organic solvents or toxic reagents, suggesting that this method is suitable for clinical applications.
Funder
JSPS Grant-in-Aid for Scientific Research on Innovative Areas
Telix Pharma Japan
The QiSS program of OPERA from the Japan Science and Technology Agency (JST), Japan
Publisher
Springer Science and Business Media LLC
Cited by
19 articles.
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