化学
电泳剂
烯丙基重排
烷基
镍
催化作用
联轴节(管道)
有机化学
组合化学
药物化学
机械工程
工程类
作者
Fei Pan,Qiao-Lin Xu,Yi Zhao,X.-Y. Liu,Na Jin,Ke‐Han He
标识
DOI:10.1002/ejoc.202400986
摘要
Fluorinated motifs are commonly found in drugs and agrochemicals. The inclusion of fluorine‐containing motifs in drug candidates during lead optimization has become a valuable strategy in pharmaceutical research and development. Significant research efforts have been dedicated to synthesizing molecules with a trifluoromethyl (CF3−) group on a stereogenic carbon. Herein, we disclose a mild and efficient nickel‐catalyzed reductive cross‐coupling between α‐trifluoromethyl alkyl bromides and allylic sulfones, enabling the efficient synthesis of α‐trifluoromethyl homoallylic alkanes. This reaction featuring base‐free, mild conditions, a broad substrate scope, and high functional group tolerance. The synthetic versatility of this approach is further underscored by its successful application in the late‐stage functionalization of a range of drug molecules. Our preliminary mechanistic study suggests that this allylation process operates through a radical intermediate.
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