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1,1-Difluoroethyl chloride (CH3CF2Cl), a novel difluoroalkylating reagent for 1,1-difluoroethylation of arylboronic acids†
RSC Advances ( IF 3.9 ) Pub Date : 2019-09-09 00:00:00 , DOI: 10.1039/c9ra06406k
Jianchang Liu 1 , Jida Zhang 1 , Chaolin Wu 1 , Hefu Liu 1 , Hui Liu 1 , Fenggang Sun 1 , Yueyun Li 1 , Yuying Liu 1 , Yunhui Dong 1 , Xinjin Li 1, 2
Affiliation  

1,1-Difluoroethylated aromatics are of great importance in medicinal chemistry and related fields. 1,1-Difluoroethyl chloride (CH3CF2Cl), a cheap and abundant industrial raw material, is viewed as an ideal 1,1-difluoroethylating reagent, but the direct introduction of the difluoroethyl (CF2CH3) group onto aromatic rings using CH3CF2Cl has not been successfully accomplished. Herein, we disclose a nickel-catalyzed 1,1-difluoroethylation of arylboronic acids with CH3CF2Cl for the synthesis of (1,1-difluoroethyl)arenes.

中文翻译:

1,1-二氟乙基氯 (CH3CF2Cl),一种用于芳基硼酸 1,1-二氟乙基化的新型二氟烷基化试剂†

1,1-二氟乙基化芳烃在药物化学及相关领域具有重要意义。1,1-二氟乙基氯(CH 3 CF 2 Cl)是一种廉价且丰富的工业原料,被视为理想的1,1-二氟乙基化试剂,但将二氟乙基(CF 2 CH 3)基团直接引入芳烃使用 CH 3 CF 2 Cl 的环尚未成功完成。在此,我们公开了一种镍催化的芳基硼酸与 CH 3 CF 2 Cl 的 1,1-二氟乙基化反应,用于合成 (1,1-二氟乙基)芳烃。
更新日期:2019-09-09
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