Methyl 4-bromobenzoate → Methyl 4-[(3,5-difluorophenyl)methylamino]benzoate

온도

100 °C

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.

ORD 기록

ord-e2f4bb7b7a8a4f84a94e64c143c99234

출처 데이터셋

750 AstraZeneca ELN dataset

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