A novel and efficient synthesis of 3-aminomethyl-N-tosyl-indazoles

作者:Kylmala Tuula; Hamalainen Antti; Kuuloja Noora; Tois Jan*; Franzen Robert
来源:Tetrahedron, 2010, 66(46): 8854-8861.
DOI:10.1016/j.tet.2010.09.069

摘要

A practical and environmentally friendly synthesis of 3-aminomethyl-N-tosyl-indazoles is developed. The in situ formed vinyl azines are reacted with amines to furnish amino functionalized anti-hydrazones in excellent yields. Subsequent copper-catalyzed cyclization at ambient temperature is effective and desired compounds are obtained in short reaction times. Also, the formation of bisindazoles is presented for the first time.

  • 出版日期2010-11-13