反应方程式
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)cc1参与物
7
反应条件
- 温度
- 100 °C
实验过程
methyl 4-bromobenzoate (1 g, 4.65 mmol), (3,5-difluorophenyl)methanamine (1.100 mL, 9.30 mmol) and Cesium carbonate (1.515 g, 4.65 mmol) were mixed in toluene (4 mL) and degassed by bubbling nitrogen through solution. Palladium acetate (0.052 g, 0.23 mmol) and rac-2,2'-Bis(diphenylphosphino)-1,1'-binaphthyl (0.203 g, 0.33 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 identity of product was doubtful but it was already used in exp 60-68.
来源与证据
- ORD记录
- ord-e2f4bb7b7a8a4f84a94e64c143c99234
- 来源数据集
- 750 AstraZeneca ELN dataset
- 原始链接
- 查看来源
关联笔记
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