Synthesis of 18F-difluoromethylarenes using aryl boronic acids, ethyl bromofluoroacetate and [18F]fluoride†
Jeroen B. I. Sap,Thomas C. Wilson,Choon Wee Kee,Natan J. W. Straathof,Christopher W. am Ende,Paramita Mukherjee,Lei Zhang,Christophe Genicot,Véronique Gouverneur
Chemical Science Pub Date : 01/29/2019 00:00:00 , DOI:10.1039/C8SC05096A
Abstract

Herein, we report the radiosynthesis of 18F-difluoromethylarenes via the assembly of three components, a boron reagent, ethyl bromofluoroacetate, and cyclotron-produced non-carrier added [18F]fluoride. The two key steps are a copper-catalysed cross-coupling reaction, and a Mn-mediated 18F-fluorodecarboxylation.

Graphical abstract: Synthesis of 18F-difluoromethylarenes using aryl boronic acids, ethyl bromofluoroacetate and [18F]fluoride