Direct Synthesis of Polysubstituted Aluminoisoxazoles and Pyrazoles by a Metalative Cyclization

作者:Jackowski Olivier; Lecourt Thomas; Micouin Laurent*
来源:Organic Letters, 2011, 13(20): 5664-5667.
DOI:10.1021/ol202389u

摘要

Alumino-heteroles are obtained from simple precursors in a fully chemo- and regioselective manner by a metalative cyclization. The carbon-aluminum bond is still able to react further with several electrophiles, without the need of transmetalation. This synthetic route provides a novel entry to heterocyclic organoaluminum reagents as well as a straightforward access to 3,4,5-trisubstituted isoxazoles and 1,3,4,5-tetrasubstituted pyrazoles.

  • 出版日期2011-10-21