Triple CH functionalization: Palladium‐catalyzed synthesis of benzofurans and coumarins by reacting phenols and unactivated olefins is described. The reaction comprises sequential CH functionalization and shows diverse functional group compatibility. Preliminary mechanistic studies shed light into the possible mechanisms.
Unactivated olefins usually react poorly in conventional alkenylation reactions. Their introduction via C-H activation is limited to aromatic acids. Herein, we disclose a C-H functionalization protocol of aromatic amines with unactivated olefins, which shows exclusive allylic selectivity for the distal ring of the biphenyl system by exploiting a readily available cobalt(II) catalyst. The allylation
An economical approach to α‐CF3‐substituted ketones, which are important intermediates in synthetic and medicinal chemistry, employs olefins and the readily available Langlois reagent (CF3SO2Na). The reaction is operationally simple, proceeds at room temperature, and exhibits an excellent tolerance toward a wide variety of functional groups.
一种经济的方法,以α-CF 3 -取代的酮,这是在合成和药物化学的重要中间体,采用烯烃和容易得到的试剂朗格卢瓦(CF 3 SO 2 Na)的。该反应操作简单,在室温下进行,并且对多种官能团表现出优异的耐受性。
Design and Scalable Synthesis of
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‐Alkylhydroxylamine Reagents for the Direct Iron‐Catalyzed Installation of Medicinally Relevant Amines**
and other biologically active small molecules. Herein, we report their direct synthesis from alkenes through an aminative difunctionalization reaction enabled by iron catalysis. A family of ten novel hydroxylamine‐derived aminating reagents were designed for the installation of several medicinally relevant amine groups, such as methylamine, morpholine and piperazine, through the aminochlorination of