Modular Synthesis of Enantioenriched 1,1,2-Triarylethanes by an Enantioselective Arylboration and Cross-Coupling Sequence
Modular Synthesis of Enantioenriched 1,1,2-Triarylethanes by an Enantioselective Arylboration and Cross-Coupling Sequence
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通过对映选择性芳基硼化和交叉偶联序列模块化合成对映富集的 1,1,2-三芳基乙烷
DOI：
10.1021/acscatal.7b00300
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发表时间：
2017-04-01
期刊：
影响因子：
12.9
通讯作者：
Liao, Jian
中科院分区：
文献类型：
--
作者：
Chen, Bin;Cao, Peng;Liao, Jian
以手性亚砜-膦(SOP)为配体，实现了铜/钯催化的苯乙烯酮与芳基/烯基碘的不对称硼化偶联反应。容易制备对映体富集型1，1-二芳基乙基和β-芳基高烯丙基硼酸酯。将芳基硼化和随后的Pd催化的Suzuki-Miyaura交叉偶联相结合的简化过程使得对映体富集型1，1，2-三芳基乙烷的模块组装成为可能，其中包括两个具有重要医学意义的手性小分子靶标。
An enantioselective Cu/Pd-catalyzed borylative coupling of styrenes with aryl/alkenyl iodides was realized using a chiral sulfoxide-phosphine (SOP) ligand. Enantioenriched 1,1-diarylethyl and beta-arylhomoallylic boronates are readily prepared. A streamlined procedure merging arylboration and subsequent Pd-catalyzed Suzuki-Miyaura cross-coupling enables the modular assembly of enantioenriched 1,1,2-triarylethanes, including two medicinally important chiral small-molecule targets.