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Rh‐Catalyzed Carboxylates Directed C–H Activation for the Synthesis of ortho‐Carboxylic 2‐Arylethenesulfonyl Fluorides: Access to Unique Electrophiles for SuFEx Click Chemistry
European Journal of Organic Chemistry ( IF 2.5 ) Pub Date : 2018-08-13 , DOI: 10.1002/ejoc.201800762
Shi-Meng Wang 1 , Balakrishna Moku 1 , Jing Leng 1 , Hua-Li Qin 1
Affiliation  

A carboxylic ester directed monoselective coupling of sp2 C–H bonds with ethenesulfonyl fluoride (ESF) was achieved by using a RhIII catalyst. This protocol gives access to a class of ortho‐carboxylic‐functionalized 2‐arylethenesulfonyl fluorides. The versatile and unique properties of carboxylic groups will significantly improve the capability of using 2‐arylethenesulfonyl fluorides as covalent probes and in drug discovery.
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中文翻译:

Rh催化的羧酸盐指示C–H活化,用于合成邻羧酸2-芳烷基磺酰氟:SuFEx Click化学方法获得独特的亲电试剂

通过使用Rh III催化剂,可以实现羧酸酯定向的sp 2 C–H键与乙磺酰氟(ESF)的单选择性偶联。通过该协议,可以访问一类羧基功能化的2-芳烷基磺酰氟。羧基的通用性和独特性将显着提高使用2-芳烷基磺酰氟作为共价探针和进行药物发现的能力。
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更新日期:2018-08-13
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