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Short Paper | Regular issue | Vol 91, No. 4, 2015, pp.815-823
Published online, 26th February, 2015
DOI: 10.3987/COM-14-13126
Domino [3+2+1] Heteroannulation for Stereoselective Synthesis of Anti-Pyrazolo[3,4-d][1,3]oxazines

Yi Ning, Wei Fan, Wen-Juan Hao, Mu-Yan Sun, Bo Jiang,* Shu-Jiang Tu,* and Guigen Li*

*Department of Chemistry & Biochemistry, Texas Tech University, Lubbock, TX 79409-1061, U.S.A.


A novel three-component domino reaction of arylglyoxals with pyrazol-5-amines in HOAc has been developed, providing an efficient and stereoselective access to polysubstituted anti-pyrazolo[3,4-d][1,3]oxazines in a intermolecular manner. Features of this strategy include mild conditions, convenient one-pot operation, and excellent stereoselectivity, which make highly attractive.