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Efficient stereoselective synthesis of benzoxazines via copper-catalyzed three-component coupling reactions
Authors:Xiaobing Xu
Affiliation:Institute of medicinal chemistry, Shanghai Key Laboratory of Green Chemistry and Chemical Processes, Department of Chemistry, East China Normal University, 3663 North Zhongshan Road, Shanghai 200062, PR China
Abstract:A convenient one-pot synthesis of 1,4-benzoxazines via three-component coupling and subsequent O-cyclization is reported. The present reaction provides an efficient protocol to functionalized 1,4-benzoxazine derivatives in good to high yields from aldehydes, amines and alkynes. Furthermore, the O-annulation process is completely regio- and stereoselective, only the six-membered rings and its Z-isomers were obtained.
Keywords:Copper catalyst   Benzoxazines   Three-component couplings   One-pot synthesis
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