Department of Chemistry, University of Utah, 315 South 1400 East, Salt Lake City, Utah 84102, USA.
Org Lett. 2012 Apr 20;14(8):2026-9. doi: 10.1021/ol300534j. Epub 2012 Apr 2.
An easy and expeditious route to substituted piperidines is described. A Ni-phosphine complex was used as catalyst for [4 + 2] cycloaddition of 3-azetidinone and alkynes. The reaction has broad substrate scope and affords piperidines in excellent yields and excellent regioselectivity. In the reaction of an enantiopure azetidinone, complete retention of stereochemistry was observed.
描述了一种简便快捷的取代哌啶合成路线。镍-膦配合物被用作催化剂,促进 3-氮杂环丁酮和炔的[4+2]环加成反应。该反应具有广泛的底物范围,能够以优异的收率和区域选择性得到哌啶。在对映体纯氮杂环丁酮的反应中,观察到立体化学完全保持。