Graduate School of Pharmaceutical Sciences, Kyoto University, Sakyo-ku, Kyoto 606-8501, Japan.
J Org Chem. 2010 Jun 4;75(11):3831-42. doi: 10.1021/jo100544v.
Palladium(0)-catalyzed cyclization of bromoallenes, propargyl chlorides, and carbonates bearing hydroxy and benzamide groups as internal nucleophiles stereoselectively provides functionalized tetrahydrofuran. Cyclization reactivity is dependent on the relative configuration of the benzamide and leaving groups, and on the nature of the leaving groups. This bis-cyclization was used as the key step in a short total synthesis of pachastrissamine, which is a biologically active marine natural product.
钯(0)催化的溴代丙二烯、炔丙基氯化物和带有羟基和苯甲酰胺基团的碳酸酯的环化反应,作为内部亲核试剂,立体选择性地提供了功能化的四氢呋喃。环化反应的活性取决于苯甲酰胺和离去基团的相对构型,以及离去基团的性质。这种双环化反应被用作短全合成帕沙司他嗪的关键步骤,帕沙司他嗪是一种具有生物活性的海洋天然产物。