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Facile Aza-Michael Additions of Uracil Derivatives to Acrylates

Journal 2012 · IF 0.633 · 发表于 2012 年 2 月 1 日
作者: Shuguang Zhou,Mingxia Xu,Siyu Ye,Dashuai Li,Jing Xu,Pei Mao,Jing Xiong
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摘要

24 Aza-Michael adducts were synthesised in moderate to excellent yields by the addition of 5-substituted uracils to acrylates with ethylamine as a catalyst. Many of the adducts were obtained in almost quantitive yield without column chromatography. The procedure provideded an efficient approach to the synthesis of N-1 uracil adducts using acrylates as acceptors. The structures of the compounds were determined by 1H NMR, 13C NMR, mass spectra and X-ray crystallography analyses. The uracil unit is present in DNA and related natural products and has a broad spectrum of biological activity.