反応式
CCOC(=O)c1cc2c(Br)cccc2o1.c1ccc(CN2CCNCC2)cc1>C1COCCO1.CC(C)c1cc(C(C)C)c(-c2ccccc2P(C2CCCCC2)C2CCCCC2)c(C(C)C)c1.O=C(/C=C/c1ccccc1)/C=C/c1ccccc1.O=C(/C=C/c1ccccc1)/C=C/c1ccccc1.O=C(/C=C/c1ccccc1)/C=C/c1ccccc1.O=C([O-])[O-].[Cs+].[Cs+].[Pd].[Pd]>CCOC(=O)c1cc2c(N3CCN(Cc4ccccc4)CC3)cccc2o1参加物
反応物 2
生成物 1
試薬・触媒・溶媒 4
反応条件
- 温度
- 95 °C
実験手順
20/10 2009 10:10:14 +0200 To ethyl 4-bromobenzofuran-2-carboxylate (2.50 g, 9.29 mmol) and 1-benzylpiperazine (1.776 mL, 10.22 mmol) in dry degassed dioxane (30 mL) were added Cesium carbonate (3.94 g, 12.08 mmol), 2-Dicyclohexylphosphino-2',4',6'-triisopropylbiphenyl (0.443 g, 0.93 mmol) and Tris(dibenzylideneacetone)dipalladium(0) (0.425 g, 0.46 mmol) under argon and the reaction heated at 95°C o/n. All starting material consumed. The crude solution was pooled with the corresponding solution in EN03307-46 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 chrom. (SiO2; Heptane/EtOAc 70/30) to give 3.05 g (50%) of the product as a yellow solid.
出典と根拠
- ORDレコード
- ord-971fd86c0ca2434fb005b5350f485988
- 出典データセット
- 750 AstraZeneca ELN dataset
- 元リンク
- 出典を表示
関連ノート
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