Direct cyclopropanation of activated N-heteroarenes via site- and stereoselective dearomative reactions
Direct cyclopropanation of activated N-heteroarenes via site- and stereoselective dearomative reactions
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DOI：
10.1039/c9sc06369b
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发表时间：
2020-02-14
期刊：
影响因子：
8.4
通讯作者：
Yoo, Eun Jeong
中科院分区：
文献类型：
--
作者：
Lee, Jiyoun;Ko, Donguk;Yoo, Eun Jeong
通过将硫叶立德脱芳加成到活化的N-杂芳烃上，完成了不同的环丙烷化反应。通过喹啉鎓两性离子的直接环丙烷化获得了一系列具有生物学意义的分子骨架。此外，在1,4-脱芳反应中使用硫叶立德作为手性亲核试剂，开发了一种光学富集环丙烷稠合杂环的直接合成路线。
A divergent cyclopropanation reaction has been accomplished via the dearomative addition of sulfur ylides to activated N-heteroarenes. A series of biologically significant molecular skeletons was obtained by the direct cyclopropanation of quinolinium zwitterions. Furthermore, a straightforward synthetic route to optically enriched cyclopropane-fused heterocycles was developed using sulfur ylides as chiral nucleophiles in the 1,4-dearomative reaction.