Department of Chemistry, University of Liverpool, Liverpool L69 7ZD, UK.
Org Lett. 2011 Jan 21;13(2):268-71. doi: 10.1021/ol102756m. Epub 2010 Dec 16.
A wide range of multisubstituted 1-indanones of potential pharmaceutical use were synthesized in a one-pot fashion in moderate to excellent yields via palladium catalysis in ethylene glycol. The Heck reaction first installs an enol functionality on the aromatic ring; this is followed by an ethylene glycol promoted aldol-type annulation with a neighboring carbonyl group, resulting in the formation of various 1-indanones.
通过钯催化在乙二醇中一锅法合成了具有潜在药用价值的多种取代 1-茚酮,产率中等至优秀。Heck 反应首先在芳环上安装烯醇官能团;随后与相邻的羰基进行乙二醇促进的 aldol 型环化反应,生成各种 1-茚酮。