【作者】 罗京华； 贺峥杰；

【Author】 Jinghua Luo;Zhengjie He;Department of Chemistry,University of Nankai;

【机构】 南开大学化学学院；

【摘要】 异噁唑啉N-氧化合物是构建具有重要生物活性的天然产物的重要骨架,该类化合物外消旋^[1]与不对称^[2]的合成方法受到了有机化学家广泛的关注。最近,我们课题组^[3]报道了叔膦催化下,MBH烯丙基碳酸酯与硝基烯的[4+1]环化反应,以中等至以上的收率合成了多取代异噁唑啉N-氧化合物。基于对路易斯碱催化的环化反应的研究,我们又实现了手性胺催化下,MBH醋酸酯与硝基烯的不对称[4+1]环化反应,该反应通过原位生成的氮叶立德中间体,高对映选择性地合成了异噁唑啉N-氧化合物（Fig.1）。更多还原

【Abstract】 Isoxazoline N-oxides have been regarded as an important class of building blocks for the construction of biologically active molecules and complex natural products.Owing to their importance in organic synthesis,different approaches towards the synthesis of isoxazoline N-oxides have been developed in a racemic or an asymmetric fashion.As part of our continuous efforts in developing new Lewis-Base-catalyzed annulation reactions,we herein present the first example of chiral amine-catalyzed nitrogen ylide initiated asymmetric[4+1]annulation between Morita-Baylis-Hillman(MBH) acetates and nitroalkenes.更多还原