通过氯化亚铜辅助的亲核芳香族溴代脱碘反应进行无载体添加的放射性溴化。

No-carrier-added radiobromination via cuprous chloride-assisted nucleophilic aromatic bromodeiodination.

作者信息

Moerlein S M, Hwang D R, Welch M J

机构信息

Edward Mallinckrodt Institute of Radiology, Washington University School of Medicine, St. Louis, MO 63110.

出版信息

Int J Rad Appl Instrum A. 1988;39(5):369-72. doi: 10.1016/0883-2889(88)90064-0.

DOI:10.1016/0883-2889(88)90064-0

PMID:2840411

Abstract

Cuprous chloride-assisted aromatic bromodeiodination was investigated as a regioselective no-carrier-added labelling technique. Using 77Br-, CuCl and simple iodinated aromatic substrates in DMSO, radiochemical yields ranged from 60 to 90% after 30 min at 135 degrees C. The methodology described here holds potential for the convenient labelling of radiopharmaceuticals with 75Br, 76Br or 77Br.

摘要

氯化亚铜辅助的芳基溴脱碘反应作为一种区域选择性无载体添加标记技术进行了研究。在二甲基亚砜中使用(^{77}Br^-)、氯化亚铜和简单的碘化芳基底物，于(135^{\circ}C)反应(30)分钟后，放射化学产率在(60%)至(90%)之间。本文所述方法具有用(^{75}Br)、(^{76}Br)或(^{77}Br)方便地标记放射性药物的潜力。