A Synthesis of “Dual Warhead” β-Aryl Ethenesulfonyl Fluorides and One-Pot Reaction to β-Sultams
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- 作者：Praveen K. Chinthakindi ; Kimberleigh B. Govender ; A. Sanjeeva Kumar ; Hendrik G. Kruger ; Thavendran Govender ; Tricia Naicker ; Per I. Arvidsson
- 刊名：Organic Letters
- 出版年：2017
- 出版时间：February 3, 2017
- 年：2017
- 卷：19
- 期：3
- 页码：480-483
- 全文大小：335K
- ISSN：1523-7052
文摘
Herein, we report an operationally simple, ligand- and additive-free oxidative boron-Heck coupling that is compatible with the ethenesulfonyl fluoride functional group. The protocol proceeds at room temperature with chemoselectivity and E-isomer selectivity and offers facile access to a wide range of β-aryl/heteroaryl ethenesulfonyl fluorides from commercial boronic acids. Furthermore, we demonstrate a “one-pot click” reaction to directly transform the products to aryl-substituted β-sultams.