Laboratory for Organic & Microwave-Assisted Chemistry (LOMAC), Department of Chemistry, University of Leuven (KU Leuven), Celestijnenlaan 200F, B-3001, Leuven, Belgium.
Org Biomol Chem. 2014 Mar 21;12(11):1741-50. doi: 10.1039/c3ob42221f.
Cationic gold-catalyzed cycloisomerizations of propargylureas, derived in situ from secondary propargylamines and aryl or alkyl isocyanates, have been studied. The reaction outcome was found to be different from what was previously observed for the tosyl isocyanate-derived ureas in terms of both regio- and chemoselectivity. As a result, the current protocol offers efficient access to the 3,4-dihydropyrimidin-2(1H)-one core through the 6-endo-dig N-cyclization.
研究了从仲炔丙胺和芳基或烷基异氰酸酯原位衍生的炔丙基脲的阳离子金催化环异构化反应。发现反应结果在区域和化学选择性方面与以前观察到的对甲苯磺酰基异氰酸酯衍生的脲不同。因此，该方案通过 6-endo-dig N-环化提供了高效构建 3,4-二氢嘧啶-2(1H)-酮核心的途径。
