反応式
COC(=O)c1ccc(Br)cc1.NCc1cc(F)cc(F)c1>CC(=O)O.CC(=O)O.Cc1ccccc1.O=C([O-])[O-].[Cs+].[Cs+].[Pd].c1ccc(P(c2ccccc2)c2ccc3ccccc3c2-c2c(P(c3ccccc3)c3ccccc3)ccc3ccccc23)cc1>COC(=O)c1ccc(NCc2cc(F)cc(F)c2)cc1参加物
7
反応条件
- 温度
- 100 °C
実験手順
methyl 4-bromobenzoate (1.8 g, 8.37 mmol), (3,5-difluorophenyl)methanamine (1.980 mL, 16.74 mmol) and Cesium carbonate (2.73 g, 8.37 mmol) were mixed in toluene (4 mL) and degassed by bubbling nitrogen through solution. Palladium acetate (0.094 g, 0.42 mmol) and rac-2,2'-Bis(diphenylphosphino)-1,1'-binaphthyl (0.365 g, 0.59 mmol) were added and the vial was capped and heated at 100°C over 5 days. Workup by dilution with EtOAc, washing with water, then extraction with 2M HCl. The HCl extract was neutralized with 2M NaOH and extracted with EtOAc and the EtOAc phase was dried (K2CO3) and evaporated to give the crude product. The desired amine was not the compound isolated. Discarded.
出典と根拠
- ORDレコード
- ord-a50a848eea9042a19d3b9efbefd39662
- 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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