5-amino-2,4-difluoro-N-methoxybenzamide

反応条件: temp:100.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: Compound 83 (100 mg, 0.43 mmol), 5-amino-2,4-difluoro-N-methoxy-benzamide (124 mg, 0.52 mmol), Pd(OAc)2 (5 mg, 0.02 mmol), X-Phos (21 mg, 0.04 mmol), and NaOtBu (125 mg, 1.30 mmol) were suspended in dioxane (2 mL), and stirred overnight at 100° C. The reaction mixture was diluted with EtOAc/H2O, and filtered through an Extrelut column. The column was washed with EtOAc, and the filtrate was concentrated. The crude product was purified via Biotage eluting with a gradient of 0 to 10% MeOH in DCM to provide 158 (5 mg, 3% yield) as a white solid. LC-MS (M+H=397, obsd.=397). filtered through an Extrelut column The column was washed with EtOAc the filtrate was concentrated The crude product was purified via Biotage eluting with a gradient of 0 to 10% MeOH in DCM

反応条件: temp:100.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: Compound 83 (100 mg, 0.43 mmol), 5-amino-2,4-difluoro-N-methoxy-benzamide (124 mg, 0.52 mmol), Pd(OAc)2 (5 mg, 0.02 mmol), X-Phos (21 mg, 0.04 mmol), and NaOtBu (125 mg, 1.30 mmol) were suspended in dioxane (2 mL), and stirred overnight at 100° C. The reaction mixture was diluted with EtOAc/H2O, and filtered through an Extrelut column. The column was washed with EtOAc, and the filtrate was concentrated. The crude product was purified via Biotage eluting with a gradient of 0 to 10% MeOH in DCM to provide 158 (5 mg, 3% yield) as a white solid. LC-MS (M+H=397, obsd.=397). filtered through an Extrelut column The column was washed with EtOAc the filtrate was concentrated The crude product was purified via Biotage eluting with a gradient of 0 to 10% MeOH in DCM

反応条件: temp:100.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: Compound 83 (100 mg, 0.43 mmol), 5-amino-2,4-difluoro-N-methoxy-benzamide (124 mg, 0.52 mmol), Pd(OAc)2 (5 mg, 0.02 mmol), X-Phos (21 mg, 0.04 mmol), and NaOtBu (125 mg, 1.30 mmol) were suspended in dioxane (2 mL), and stirred overnight at 100° C. The reaction mixture was diluted with EtOAc/H2O, and filtered through an Extrelut column. The column was washed with EtOAc, and the filtrate was concentrated. The crude product was purified via Biotage eluting with a gradient of 0 to 10% MeOH in DCM to provide 158 (5 mg, 3% yield) as a white solid. LC-MS (M+H=397, obsd.=397). filtered through an Extrelut column The column was washed with EtOAc the filtrate was concentrated The crude product was purified via Biotage eluting with a gradient of 0 to 10% MeOH in DCM