一种用于区域选择性构建含吡唑脂肪族磺酰氟的级联反应。
A cascade reaction for regioselective construction of pyrazole-containing aliphatic sulfonyl fluorides.
作者信息
Yang Wen-Fei, Shu Tao, Chen Hong-Ru, Qin Hua-Li, Tang Haolin
机构信息
School of Chemistry, Chemical Engineering and Life Sciences; and State Key Laboratory of Advanced Technology for Materials Synthesis and Processing, Wuhan University of Technology, Wuhan 430070, China.
出版信息
Org Biomol Chem. 2022 May 4;20(17):3506-3510. doi: 10.1039/d2ob00515h.
A copper-catalyzed cascade reaction of α-diazocarbonyl compounds with ethenesulfonyl fluoride (ESF) is developed, affording a variety of highly functionalized pyrazolyl aliphatic sulfonyl fluorides in good to excellent yields (66-98%). This transformation features broad substrates, exclusive regioselectivity, high atom economy and operational simplicity, thus providing a straightforward method for the direct construction of pyrazole-containing aliphatic sulfonyl fluorides, which will provide great applicable value in medicinal chemistry and other related disciplines.
开发了一种铜催化的α-重氮羰基化合物与乙烯基磺酰氟（ESF）的串联反应，以良好至优异的产率（66-98%）得到了多种高度官能化的吡唑基脂肪族磺酰氟。该转化具有底物范围广、区域选择性专一、原子经济性高和操作简便等特点，从而为直接构建含吡唑的脂肪族磺酰氟提供了一种直接的方法，这将在药物化学和其他相关学科中具有巨大的应用价值。
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