Beyond the rapid achievements of therapeutic heterobifunctional molecules, some recent efforts have focused on constructing heterotrifunctional molecules, aiming at developing more potent and selective therapeutic agents or emerging additional functions to heterobifunctional molecules. However, the synthesis of these complex molecules requires a specific design and lengthy steps. We have developed a two-step strategy for the modular construction of heterotrifunctional molecules, enabled by the sustainable and convenient iodosulfonylation of allenes followed by S_N2′-selective amination. This strategy successfully incorporates a broad range of biologically active molecules, labeling them with a fluorescent group. The applications of the obtained compounds in selective protein labeling, subcellular imaging, and targeted inhibition of tumor cells make this strategy highly appealing.

中文翻译：

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通过烯的碘磺酰化和随后的胺化实现异三功能分子的模块化组装


除了治疗性异双功能分子的快速成就外，最近的一些工作还集中在构建异三功能分子上，旨在开发更有效和选择性的治疗剂或为异双功能分子提供附加功能。然而，这些复杂分子的合成需要特定的设计和漫长的步骤。我们开发了一种用于异质三功能分子模块化构建的两步策略，通过可持续和方便的等位烯碘磺酰化，然后进行 S_N2′ 选择性胺化。该策略成功地掺入了广泛的生物活性分子，并用荧光基团标记它们。所获得的化合物在选择性蛋白质标记、亚细胞成像和肿瘤细胞靶向抑制中的应用使该策略极具吸引力。