通过炔烃的银介导直接放射性氟化反应，使用无载体添加的[F]AgF制备[F]链烯基氟化物。

Preparation of [F]Alkenyl Fluorides Using No-Carrier-Added [F]AgF via Silver-Mediated Direct Radiofluorination of Alkynes.

作者信息

Gao Xinyan, Gong Kehao, Wang Mingwei, Xu Bo, Han Junbin

机构信息

Institute of Radiation Medicine, Fudan University, Xietu Road 2094, Shanghai 200032, China.

Department of Nuclear Medicine, Fudan University Shanghai Cancer Center, 270 Dong'An Road, Shanghai 200032, China.

出版信息

Org Lett. 2022 Sep 9;24(35):6438-6442. doi: 10.1021/acs.orglett.2c02553. Epub 2022 Aug 28.

DOI:10.1021/acs.orglett.2c02553

PMID:36030419

Abstract

We have developed a versatile method for the radiosynthesis of [F]alkenyl fluorides using no-carrier-added [F]AgF via the silver-mediated direct radiofluorination of alkynes. A variety of electron-deficient internal alkynes were compatible with this strategy and gave the desired product in good regioselectivity and RCY. This method could also be applied to the late-stage radiofluorination and showed potential in nuclear medicine development.

摘要

我们已经开发出一种通用方法，通过炔烃的银介导直接放射性氟化反应，使用无载体添加的[F]AgF进行[F]烯基氟化物的放射性合成。多种缺电子内炔烃与该策略兼容，并以良好的区域选择性和放射性化学产率得到所需产物。该方法还可应用于后期放射性氟化反应，并在核医学发展中显示出潜力。