Due to its unique three-dimensional (3D) configuration and great application potential in medicinal chemistry and synthetic community, chemists have been pursuing concise and efficient methods to synthesize C3 spirocyclic indoline derivatives. In this work, a dearomatization–spirocyclization–nucleophilic addition tandem approach was developed to realize the synthesis of 2-phosphonylated C3 spirocyclic indolines with indolyl-ynones and phosphine oxides as reactants; mild conditions, broad substrate scope, and good yields are characteristics of this transformation.

中文翻译：

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通过吲哚基-炙酮与磷化氢的脱芳烃化-螺环化-亲核加成串联方法合成 2-膦酰化 C3 螺环吲哚啉


由于其独特的三维 （3D） 构型以及在药物化学和合成界的巨大应用潜力，化学家们一直在寻求简洁有效的方法来合成 C3 螺环吲哚啉衍生物。在这项工作中，开发了一种脱芳烃化-螺环化-亲核加成串联方法，以实现以吲哚基-伊酮和磷化氢氧化物为反应物的 2-膦酰化 C3 螺环吲哚啉的合成;温和的条件、广泛的底物范围和良好的产量是这种转变的特点。