Ligandless Copper‐Catalyzed Carboborylation of Heteroatom‐Substituted Alkynes,Advanced Synthesis & Catalysis

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Ligandless Copper‐Catalyzed Carboborylation of Heteroatom‐Substituted Alkynes
Advanced Synthesis & Catalysis ( IF 4.4 ) Pub Date : 2018-07-26 , DOI: 10.1002/adsc.201800656
Shiwen Liu ₁ , Xiaojun Zeng ₁ , Bo Xu ₁

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We have developed an efficient ligand‐free copper‐catalyzed regio‐ and stereoselective carbo‐borylation of heteroatom‐substituted internal alkynes using bis(pinacolato)diboron as boron source and alkyl halides as an electrophile. Both chemical yields and functional group tolerance are excellent. Our method provides an efficient synthesis of tri‐ and tetra‐substituted alkenylboronates which could be further transformed to highly substituted alkenes via subsequent cross‐coupling reactions in one pot.

中文翻译：

杂原子取代的炔烃的无配体铜催化碳硼化

我们已经开发了一种高效的，无杂原子取代的内部炔烃的无配体铜催化的区域和立体选择性碳硼化反应，使用双（频哪醇）二硼烷作为硼源，卤代烷作为亲电体。化学产率和官能团耐受性均优异。我们的方法提供了三取代和四取代的烯基硼酸酯的有效合成方法，可通过随后在一个罐中进行交叉偶联反应将其进一步转化为高度取代的烯烃。

更新日期：2018-07-26

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