Direct synthesis of N_(2)-unprotected five-memberedcyclic guanidines by regioselective[3+2]annulation of aziridines and cyanamides  

作　　者：Chuan-Chuan Wang Xin-Lu Wang Qing-Ling Zhang Juntao Liu Zhi-Wei M Zhi-Jing Liu Ya-Jing Chen 

机构地区：[1]School of Pharmaceutical Sciences,Key Laboratory of Advanced Drug Preparation Technologies,Ministry of Education of China,Co-Innovation Center of Henan Province for New Drug R&D and Preclinical Safety,Zhengzhou University,100 Science Avenue,Zhengzhou 450001,Henan,China [2]Faculty of Science,Livestock Product Quality Inspection Institute,Henan University of Animal Husbandry and Economy,No.146 Yingcai Street,Zhengzhou 450044,Henan,China

出　　处：《Organic Chemistry Frontiers》2022年第6期1574-1579,共6页有机化学前沿（英文）

基　　金：support from the Natural Science Foundation of Henan Province(grant no.212300410152);the Key Scientific and Technological Project of Henan Province(grant no.212102110439);Henan University of Animal Husbandry and Economy(grant no.2019HNUAHEDF011 and XKYCXJJ2020006);the Key Scientific Research Project for Colleges and Universities of Henan Province(grant no.22B150005)。

摘　　要：A novel and efficient[3+2]annulation of 2-substituted aziridines and N-tosyl cyanamides via a dominoregioselective ring-opening/5-exo-dig cyclization procedure has been developed,allowing the directpreparation of N_(2)-unprotected five-membered cyclic guanidines in good to excellent yields under mildconditions without metals and strong bases.Moreover,the highly biologically interesting urea analoguescould also be conveniently obtained via hydrolysis of the produced guanidines.

关 键 词：membered protected GUANIDINE 

分 类 号：O62[理学—有机化学]