反応 #193

ord-09c188bd82d940b1aa9d4223b96f551d

反応方程式

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
収率 64.4%

溶媒

反応条件

温度
95°CELSIUS

実験手順

22/04 2009 09:43:42 +0200 To ethyl 7-bromobenzofuran-2-carboxylate (0.095 g, 0.35 mmol) and 1-(5-(2-(piperazin-1-yl)ethyl)indolin-1-yl)ethanone (0.101 g, 0.37 mmol) (from EN02198-74) in dry degassed dioxane (1.5 mL) were added Cesium carbonate (0.150 g, 0.46 mmol), 2-Dicyclohexylphosphino-2',4',6'-triisopropylbiphenyl (0.017 g, 0.04 mmol) and Tris(dibenzylideneacetone)dipalladium(0) (0.016 g, 0.02 mmol) under argon and the reaction heated at 95°C for 5.5h. 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 0.105 g of the product as a yellow solid.

出典

750 AstraZeneca ELN dataset