A Rh^III-catalyzed C(sp²)–H N-heteroarylation and esterification cascade of aryl carboxylic acids with N-heteroaromatic boronates and 1,2-dichloroethane in a one-pot synthesis has been disclosed. The strong coordinating ability of ortho- and meta-substituted pyridine boronates and pyrazoles as well as unsubstituted pyrimidine allows them to serve as the coupling partners. This protocol allows late-stage modification of the key precursor of roflumilast and compounds of pharmaceutical interest, which highlights the potential application of this synthetic method.

中文翻译：

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有机硼试剂和 1,2-二氯乙烷在一锅法合成中 RhIII 催化羧酸的 C-H N-杂芳基化和酯化级联反应

已经公开了在一锅合成中芳基羧酸与N-杂芳族硼酸酯和 1,2-二氯乙烷的 Rh ^III催化的 C(sp ² )-H N-杂芳基化和酯化级联反应。邻位和间位取代的吡啶硼酸盐和吡唑以及未取代的嘧啶具有很强的配位能力，可以作为偶联配偶体。该协议允许对罗氟司特的关键前体和药物感兴趣的化合物进行后期修改，这突出了这种合成方法的潜在应用。