The prevalence of naphthalene compounds in biologically active natural products, organic ligands and approved drugs has motivated the development of efficient strategies for their selective synthesis. C-H functionalization of naphthalene has been frequently used, but mainly focus on two-component reaction, while multiple-component C-H functionalization for the synthesis of naphthalene compounds has thus far proven elusive. Herein, we disclose a versatile three-component protocol for the modular synthesis of multifunctional naphthalenes from readily available simple naphthalenes, olefins and alkyl bromides via P(III)-assisted ruthenium catalyzed remote C-H functionalization. This protocol not only tolerates various functional groups, but can be applied to many natural product and drug derivatives, including three-component reaction with two different bioactive molecules. Mechanism studies indicated that the utilization of tertiary phosphines as auxiliary groups is the key to achieving the three-component free radical reaction.

中文翻译：

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钌催化萘的三组分串联远程 C-H 官能团化：多功能萘的模块化和简洁合成


萘化合物在生物活性天然产物、有机配体和已批准药物中的普遍存在，推动了其选择性合成的有效策略的开发。萘的 C-H 官能团化已被广泛使用，但主要集中在双组分反应上，而用于合成萘化合物的多组分 C-H 官能团化迄今已被证明难以捉摸。在此，我们公开了一种多功能的三组分方案，用于通过 P（III） 辅助钌催化的远程 CH 官能化从现成的简单萘、烯烃和烷基溴模块化合成多功能萘。该方案不仅耐受各种官能团，而且可应用于许多天然产物和药物衍生物，包括与两种不同生物活性分子的三组分反应。机理研究表明，利用叔膦作为辅助基团是实现三组分自由基反应的关键。