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采用 PhI(OAc)-介导的多米诺反应来组装含氮杂环衍生物,并评估它们的抗炎活性。

Employing a PhI(OAc)-mediated domino reaction to assemble nitrogen-containing heterocyclic derivatives and assessing their anti-inflammatory activity.

机构信息

College of Chinese Medicine, the First Affiliated Hospital, and Key Laboratory of Xin'an Medicine of the Ministry of Education, Anhui University of Chinese Medicine, Hefei, 230038, P. R. China.

Institute of Pharmaceutical Chemistry, Anhui Academy of Chinese Medicine, Hefei, 230038, P. R. China.

出版信息

Chem Commun (Camb). 2024 Nov 12;60(91):13352-13355. doi: 10.1039/d4cc03245d.

Abstract

Metal-free radical cascade synthesis of substituted pyrazole derivatives was initiated by PhI(OAc) at 23 °C. This protocol features wide functional group tolerance, a simple purification process without column chromatography, and an oxygen migration. Compound 5 demonstrated significant anti-inflammatory activity, indicating potential for therapy.

摘要

PhI(OAc)引发的无金属自由基级联合成反应可在 23°C 下合成取代吡唑衍生物。该方法具有广泛的官能团耐受性,无需柱层析即可进行简单的纯化过程,且发生了氧迁移。化合物 5 表现出显著的抗炎活性,表明其具有治疗潜力。

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