Transition metal-free Csp^(3)-Csp^(3) bond-forming reactions of N-tosylaziridines and gem-diborylalkanes  

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作  者:Pu-Zhang Zi Quan-Hong Zhao Zhan-Cai Ma Xiao-Lin Ren Xing-Bang Liu Yi-Wei Qiao Lin-Wen Wei Song Liu Yuan Huang 

机构地区:[1]Department of Medicinal Chemistry,School of Pharmacy,Xi’an Jiaotong University,Xi’an 710061,China [2]Chongqing Key Laboratory of Environmental Materials and Remediation Technologies College of Chemistry and Environmental Engineering,Chongqing University of Arts and Sciences,Chongqing 402160,China

出  处:《Green Synthesis and Catalysis》2024年第4期329-333,共5页绿色合成与催化(英文)

基  金:financial support provided by the National Natural Science Foundation of China(No.22001203).

摘  要:The incorporation of additional Csp^(3) atoms into candidate drugs may enhance their pharmacological properties.Nevertheless,it remains challenging to construct desired Csp^(3)-Csp^(3) bonds efficiently and practically.The present article reports a novel Csp^(3)-Csp^(3) bond-forming reaction of 2-aryl/alkyl substituted aziridines with gem-diborylalkanes under tranisiton metal free conditions.A wide range ofγ-gem-diboronate esters substituted amines can be accessed in good yield and regioselectivity.The results demonstrated that various aziridines could react with gem-diborylalkanes in the presence of LiTMP as the base within 15 min at ambient temperature.

关 键 词:Csp^(3)-Csp^(3)bond formation Transition metal-free N-tosylaziridines gem-diborylalkanes Ring-opening reactions 

分 类 号:O62[理学—有机化学]

 

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