高价碘介导的酰苯胺的对位选择性氟化反应。

Hypervalent iodine mediated para-selective fluorination of anilides.

机构信息

The State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, Peking University, Beijing 100191, PR China.

出版信息

J Org Chem. 2013 Jan 18;78(2):728-32. doi: 10.1021/jo302099d. Epub 2012 Dec 18.

DOI:10.1021/jo302099d

PMID:23228030

Abstract

A metal-free method for the direct regioselective fluorination of anilides has been developed. In the presence of bis(tert-butylcarbonyloxy)iodobenzene (PhI(OPiv)(2)) and hydrogen fluoride-pyridine, the para-fluorination products of anilides were obtained in moderate to good yields. Because of its operational safety and the use of readily available reagents, this new procedure provides facile access to a variety of para-fluorinated anilides.

摘要

一种无需金属的方法被开发用于苯胺的直接区域选择性氟化。在双(叔丁基羰氧基)碘苯（PhI(OPiv)(2)）和氟化氢-吡啶的存在下，苯胺的对位氟化产物以中等至良好的产率得到。由于其操作安全性和使用易得的试剂，这种新方法为各种对位氟化苯胺提供了简便的途径。