铑催化羧酸与有机硼试剂及1,2-二氯乙烷在一锅合成中的C-H-杂芳基化和酯化串联反应
Rh-Catalyzed C-H -Heteroarylation and Esterification Cascade of Carboxylic Acid with Organoboron Reagents and 1,2-Dichloroethane in One-Pot Synthesis.
作者信息
Wang Huai-Wei, Wu Jia-Xue, Huang Xian-Qiang, Li Da-Cheng, Wang Su-Na, Lu Yi, Dou Jian-Min
机构信息
Shandong Provincial Key Laboratory of Chemical Energy Storage and Novel Cell Technology, School of Chemistry and Chemical Engineering, Liaocheng University, Liaocheng 252000, China.
Coordination Chemistry Institute, State Key Laboratory of Coordination Chemistry, School of Chemistry and Chemical Engineering, Nanjing University, Nanjing 210023, China.
出版信息
Org Lett. 2022 Aug 12;24(31):5704-5709. doi: 10.1021/acs.orglett.2c02075. Epub 2022 Jul 30.
A Rh-catalyzed C(sp)-H -heteroarylation and esterification cascade of aryl carboxylic acids with -heteroaromatic boronates and 1,2-dichloroethane in a one-pot synthesis has been disclosed. The strong coordinating ability of - and -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.
已公开了一种铑催化的芳基羧酸与杂芳基硼酸酯及1,2 - 二氯乙烷在一锅法合成中的C(sp)-H - 杂芳基化和酯化级联反应。β-和γ-取代的吡啶硼酸酯、吡唑以及未取代的嘧啶的强配位能力使其能够作为偶联伙伴。该方法允许对罗氟司特的关键前体及具有药物研究价值的化合物进行后期修饰，这突出了这种合成方法的潜在应用。
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