Copper(I)-catalyzed Diastereoselective Dearomative Carboborylation of Indoles
Copper(I)-catalyzed Diastereoselective Dearomative Carboborylation of Indoles
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DOI：
10.1246/cl.170825
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发表时间：
2017-12-01
影响因子：
1.6
通讯作者：
Ito, Hajime
中科院分区：
文献类型：
--
作者：
Hayama, Keiichi;Kubota, Koji;Ito, Hajime
在铜（I）催化下，首次实现了杂芳族化合物的C-B键形成脱芳碳硼基化反应。该反应包括硼基铜（I）中间体与吲哚的区域选择性加成，然后对所得烯醇化铜（I）中间体进行非对映选择性甲基化，以提供具有优异的区域和非对映选择性的带有季立体中心的相应的3-硼基-2-甲基吲哚啉。
The first C-B bond-forming dearomative carboborylation of heteroaromatic compounds has been achieved using copper(I) catalysis. This reaction includes the regioselective addition of a borylcopper(I) intermediate to indoles, followed by the diastereoselective methylation of the resulting copper(I) enolate intermediate to afford the corresponding 3-boryl-2-methylindolines bearing a quaternary stereogenic center with excellent regio- and diastereoselectivity.