反应 #192

ord-90e612e9a6744ee3af3c528f17e1b1ce

反应方程式

CCOC(=O)c1cc2cccc(Br)c2o1
CCOC(=O)c1cc2cccc(Br
CC(=O)N1CCc2cc(CCN3CCNCC3)ccc21
CC(=O)N1CCc2cc(CCN3C
CCOC(=O)c1cc2cccc(N3CCN(CCc4ccc5c(c4)CCN5C(C)=O)CC3)c2o1
CCOC(=O)c1cc2cccc(N3
收率 61.5%

溶剂

反应条件

温度
95°CELSIUS

实验过程

06/05 2009 14:53:56 +0200 To ethyl 7-bromobenzofuran-2-carboxylate (0.460 g, 1.71 mmol) and 1-(5-(2-(piperazin-1-yl)ethyl)indolin-1-yl)ethanone (0.491 g, 1.79 mmol) (from EN02198-74) in dry degassed dioxane (8 mL) were added Cesium carbonate (0.724 g, 2.22 mmol), 2-Dicyclohexylphosphino-2',4',6'-triisopropylbiphenyl (0.081 g, 0.17 mmol) and Tris(dibenzylideneacetone)dipalladium(0) (0.078 g, 0.09 mmol) under argon and the reaction heated at 95°C overnight. After cooling to rt, water and DCM were added and the layers separated. The aq phase was extracted with DCM (3x). The combined org phases were washed with water, dried (MgSO4), filtered and evaporated. The crude was purified by flash (SiO2; DCM/MeOH 95/5) to give 0.485 g (61%) of the product as a yellow solid.

来源

750 AstraZeneca ELN dataset