使用芳基硼酸、溴氟乙酸乙酯和[F]氟化物合成氟代二氟甲基芳烃。

Synthesis of F-difluoromethylarenes using aryl boronic acids, ethyl bromofluoroacetate and [F]fluoride.

作者信息

Sap Jeroen B I, Wilson Thomas C, Kee Choon Wee, Straathof Natan J W, Ende Christopher W Am, Mukherjee Paramita, Zhang Lei, Genicot Christophe, Gouverneur Véronique

机构信息

Chemistry Research Laboratory , Department of Chemistry , Oxford University , OX1 3TA Oxford , UK . Email:

Pfizer Inc., Medicine Design , Eastern Point Road, Groton, Connecticut 06340, and 1 Portland Street , Cambridge , Massachusetts 02139 , USA.

出版信息

Chem Sci. 2019 Jan 29;10(11):3237-3241. doi: 10.1039/c8sc05096a. eCollection 2019 Mar 21.

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