chloromethyl 2-methyl-2-[(2-methylpropan-2-yl)oxycarbonylamino]propanoate

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

実験手順: The title compound was prepared according to the procedure as described in Example 14 Step 2 using N-(3-(5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonamide (0.3 g, 0.61 mmol) in DMF (2.5 mL), KOH (69 mg, 0.4 mmol), and a solution of chloromethyl 2-((tert-butoxycarbonyl)amino)-2-methylpropanoate (158 mg, 0.61 mmol) in DMF (0.5 mL). The title compound was purified by a silica gel columnchromatography (PE/EtOAc (v/v)=4/1 to 3/1) and was obtained as a white solid (339 mg, 78.7%). The title compound was characterized by LC-MS and 1H NMR as shown below: The title compound was purified by a silica gel columnchromatography (PE/EtOAc (v/v)=4/1 to 3/1)

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

実験手順: The title compound was prepared according to the procedure as described in Example 17 Step 1 using 2-((tert-butoxycarbonyl)amino)-2-methylpropanoic acid (1.07 g, 5.29 mmol) in DCM (25 mL) and H2O (25 mL), NaHCO3 (1.78 g, 21.2 mmol), TBAHSO4 (0.18 g, 0.53 mmol) and a solution of chloromethyl sulfochloridate (638 μL, 6.35 mmol) in DCM (5 mL). The title compound was obtained as a white solid (1.16 g, 87.7%). The title compound was characterized by 1H NMR as shown below: The title compound was prepared

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

実験手順: The title compound was prepared according to the procedure as described in Example 17 Step 1 using 2-((tert-butoxycarbonyl)amino)-2-methylpropanoic acid (1.07 g, 5.29 mmol) in DCM (25 mL) and H2O (25 mL), NaHCO3 (1.78 g, 21.2 mmol), TBAHSO4 (0.18 g, 0.53 mmol) and a solution of chloromethyl sulfochloridate (638 μL, 6.35 mmol) in DCM (5 mL). The title compound was obtained as a white solid (1.16 g, 87.7%). The title compound was characterized by 1H NMR as shown below: The title compound was prepared

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

実験手順: The title compound was prepared according to the procedure as described in Example 14 Step 2 using N-(3-(5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonamide (0.3 g, 0.61 mmol) in DMF (2.5 mL), KOH (69 mg, 0.4 mmol), and a solution of chloromethyl 2-((tert-butoxycarbonyl)amino)-2-methylpropanoate (158 mg, 0.61 mmol) in DMF (0.5 mL). The title compound was purified by a silica gel columnchromatography (PE/EtOAc (v/v)=4/1 to 3/1) and was obtained as a white solid (339 mg, 78.7%). The title compound was characterized by LC-MS and 1H NMR as shown below: The title compound was purified by a silica gel columnchromatography (PE/EtOAc (v/v)=4/1 to 3/1)

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

実験手順: The title compound was prepared according to the procedure as described in Example 17 Step 1 using 2-((tert-butoxycarbonyl)amino)-2-methylpropanoic acid (1.07 g, 5.29 mmol) in DCM (25 mL) and H2O (25 mL), NaHCO3 (1.78 g, 21.2 mmol), TBAHSO4 (0.18 g, 0.53 mmol) and a solution of chloromethyl sulfochloridate (638 μL, 6.35 mmol) in DCM (5 mL). The title compound was obtained as a white solid (1.16 g, 87.7%). The title compound was characterized by 1H NMR as shown below: The title compound was prepared