Research On The Y(OTf)₃-catalyzed [3+2]-Annulation Reaction Of Donor-Acceptor Aziridines With 2H-azirines

This thesis focused on the synthesis of 1,3-diazabicyclo[3.1.0]hexanes based on the[3+2]-annulation reaction of donor-acceptor aziridines with 2H-azirines.This thesis consists of the following two parts.Chapter 1:After modified,three membered and four membered ring compounds have been fully developed in annulation reaction under Lewis acid catalysis and it is important in organic synthesis.This chapter briefly introduced the Lewis acid-catalyzed annulation reactions of the compounds bearing strained rings,such as D-A cyclopropanes,aziridines,oxiranes,cyclobutanes,were firstly summarized.Then,we introduced their different reaction mechanisms in detail and their applicants in organic synthesis.Finally,we briefly analysed the superiorities and defects of the reactions.Chapter 2:Iminazole derivatives had widespread applications in pharmaceutical agents,organic synthesis.Based on the analysis of the trait of the 2H-azirine and its application in organic synthesis,we investigated the Y(OTf)₃-catalyzed[3+2]-annulation reaction of aziridines with 2H-azirines,and developed an efficient method for the synthesis 1,3-diazabicyclo[3.1.0]hexanes.Mild conditions,high yield,excellent diastereoselectivity and facile derivatization of product revealed that this annulation reaction is useful in organic synthesis...