Gao Peng, Wang Juan, Bai Zijing, Yang Desuo, Fan Ming-Jin, Guan Zheng-Hui
Shaanxi Key Laboratory of Phytochemistry, College of Chemistry and Chemical Engineering, Baoji University of Arts and Sciences, 1 # Hi-Tech Avenue, Baoji, Shaanxi, 721013, China.
Key Laboratory of Synthetic and Natural Functional Molecule Chemistry of Ministry of Education, Department of Chemistry & Materials Science, Northwest University, 1 # Xuefu Avenue, Xi'an, Shaanxi, 710127, China.
Chem Asian J. 2017 Aug 4;12(15):1865-1868. doi: 10.1002/asia.201700503. Epub 2017 Jun 29.
A facile synthesis of 2-amino-1,3-oxazoles via Cu -catalyzed oxidative cyclization of enamines and N,N-dialkyl formamides has been developed. The reaction proceeds through an oxidative C-N bond formation, followed by an intramolecular C(sp )-H bond functionalization/C-O cyclization in one pot. This protocol provides direct access to useful 2-amino-1,3-oxazoles and features protecting-group-free nitrogen sources, readily available starting materials, a broad substrate scope and mild reaction conditions.
通过铜催化烯胺与N,N-二烷基甲酰胺的氧化环化反应，实现了2-氨基-1,3-恶唑的简便合成。该反应通过氧化C-N键形成，随后在一锅法中进行分子内C(sp³)-H键官能团化/C-O环化。此方法可直接合成有用的2-氨基-1,3-恶唑，具有无需保护基团的氮源、易得的起始原料、广泛的底物范围和温和的反应条件。
