区域选择性
铑
化学
催化作用
表面改性
功能群
药物化学
组合化学
立体化学
有机化学
物理化学
聚合物
作者
Zhong‐Tao Jiang,Jiangkun Huang,Yaxin Zeng,Fangdong Hu,Ying Xia
标识
DOI:10.1002/anie.202016258
摘要
Abstract Herein, we report a rhodium catalyzed directing‐group free regioselective C−H allylation of simple arenes. Readily available gem ‐difluorinated cyclopropanes can be employed as highly reactive allyl surrogates via a sequence of C−C and C−F bond activation, providing allyl arene derivatives in good yields with high regioselectivity under mild conditions. The robust methodology enables facile late‐stage functionalization of complex bioactive molecules. The high efficiency of this reaction is also demonstrated by the high turnover number (TON, up to 1700) of the rhodium catalyst on gram‐scale experiments. Preliminary success on kinetic resolution of this transformation is achieved, providing a promising access to enantio‐enriched gem ‐difluorinated cyclopropanes.
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