Zhu Bing-Ke, Xu Hui, Xiao Lu, Chang Xin, Wei Liang, Teng Huailong, Dang Yanfeng, Dong Xiu-Qin, Wang Chun-Jiang
College of Chemistry and Molecular Sciences, Engineering Research Center of Organosilicon Compounds & Materials, Ministry of Education, Wuhan University Wuhan Hubei 430072 P. R. China
State Key Laboratory of Organometallic Chemistry, Shanghai Institute of Organic Chemistry Shanghai 230021 China.
Chem Sci. 2023 Mar 14;14(15):4134-4142. doi: 10.1039/d3sc00118k. eCollection 2023 Apr 12.
Highly diastereo-/enantioselective assembly of 2,3-fused indolizine derivatives could be easily available through a cascade allylation/Friedel-Crafts type reaction enabled by a synergistic Cu/Ir catalysis. This designed protocol provides an unprecedented and facile route to enantioenriched indolizines bearing three stereogenic centers in moderate to high yields with excellent stereoselective control, which also featured broad substrate generality. Remarkably, four stereoisomers of the 2,3-fused indolizine products could be efficiently constructed in a predictable manner through the pairwise combination of copper and iridium catalysts. The synthetic utility of this method was readily elaborated by a gram-scale reaction, and synthetic transformations to other important chiral indolizine derivatives. Quantum mechanical explorations constructed a plausible synergetic catalytic cycle, revealed the origins of stereodivergence, and rationalized the protonation-stimulated stereoselective Friedel-Crafts type cyclization to form the indolizine products.
通过协同铜/铱催化实现的串联烯丙基化/傅克型反应,可以轻松实现2,3-稠合中氮茚衍生物的高非对映/对映选择性组装。该设计方案为构建具有三个立体中心的对映体富集的中氮茚提供了一条前所未有的便捷途径,产率适中至高,立体选择性控制优异,且底物适应性广泛。值得注意的是,通过铜和铱催化剂的成对组合,可以以可预测的方式高效构建2,3-稠合中氮茚产物的四种立体异构体。该方法的合成实用性通过克级反应以及向其他重要手性中氮茚衍生物的合成转化得以轻松展现。量子力学探索构建了一个合理的协同催化循环,揭示了立体发散的起源,并合理解释了质子化刺激的立体选择性傅克型环化反应以形成中氮茚产物的过程。