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A facile synthesis of 2-aryloxypyrimidine derivatives via a tandem reductive amination/intermolecular S_NAr sequence
Authors:Hai-feng WU  Pei-zhi ZHANG  Jun WU
Institution:1.Department of Chemistry, Zhejiang University, Hangzhou 310027, China;2.School of Biological and Chemical Engineering, Zhejiang University of Science and Technology, Hangzhou 310012, China
Abstract:A novel tandem reductive amination/intermolecular nucleophilic aromatic substitution (SNAr) sequence has been established for the synthesis of amine containing pyrimidine in formation of one carbon-oxygen and one carbon-nitrogen bonds in a one-pot fashion. Treatment of aldehyde with arylamine, 2-methanesulfonyl-4,6-dimeth-oxypyrimidine and sodium borohydride provides good overall yield. The p-toluenesulfonic acid (PTSA) can be used as activator and is generally needed in the reaction. Dioxane is the preferr...
Keywords:Reductive amination/intermolecular SNAr  C-O and C-N bonds  Amine  Pyrimidine  Herbicide  
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