N-[(3-amino-4-chlorophenyl)methyl]-2,2-dimethylpropanamide

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 described in step-1 of Intermediate-61 by using N-(3-amino-4-chlorobenzyl)pivalamide (1.80 g), NaNO2 (0.62 g, 0.009 mmol), SnCl2.2H2O (4.2 g, 0.018 mmol) and conc. HCl (30 mL) to afford 1.5 g of the desired product. 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 described in step-2 of Intermediate-83 by using 5-(aminomethyl)-2-chlorobenzenamine (2.0 g), pivaloyl chloride (0.2 mL), TEA (2 mL) and THF (10 mL) to afford 2.0 g of the desired product. 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 described in step-2 of Intermediate-83 by using 5-(aminomethyl)-2-chlorobenzenamine (2.0 g), pivaloyl chloride (0.2 mL), TEA (2 mL) and THF (10 mL) to afford 2.0 g of the desired product. 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 described in step-1 of Intermediate-61 by using N-(3-amino-4-chlorobenzyl)pivalamide (1.80 g), NaNO2 (0.62 g, 0.009 mmol), SnCl2.2H2O (4.2 g, 0.018 mmol) and conc. HCl (30 mL) to afford 1.5 g of the desired product. 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 described in step-2 of Intermediate-83 by using 5-(aminomethyl)-2-chlorobenzenamine (2.0 g), pivaloyl chloride (0.2 mL), TEA (2 mL) and THF (10 mL) to afford 2.0 g of the desired product. 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 described in step-1 of Intermediate-61 by using N-(3-amino-4-chlorobenzyl)pivalamide (1.80 g), NaNO2 (0.62 g, 0.009 mmol), SnCl2.2H2O (4.2 g, 0.018 mmol) and conc. HCl (30 mL) to afford 1.5 g of the desired product. 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 described in step-2 of Intermediate-83 by using 5-(aminomethyl)-2-chlorobenzenamine (2.0 g), pivaloyl chloride (0.2 mL), TEA (2 mL) and THF (10 mL) to afford 2.0 g of the desired product. 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: 1,1′-Thiocarbonyldi-2-pyridone (2.12 g, 9.1 mmol) was added to a mixture of N-(3-amino-4-chlorobenzyl)-2,2-dimethyl-propionamide (2.00 g, 8.3 mmol) and DCM (60 mL) and stirred at rt for 1.5 h. The mixture was filtered over silica gel. The organic layer was concentrated to give the sub-title compound. The mixture was filtered over silica gel The organic layer was concentrated

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

実験手順: A mixture of N-(4-chloro-3-nitrobenzyl)-2,2-dimethyl-propionamide (5.92 g, 21.9 mmol), THF (150 mL) and Ra—Ni (1.50 g) was stirred for 2 days at RT under a hydrogen atmosphere (3.0 bar). The catalyst was removed by filtration and the mixture was concentrated. The crude was purified by chromatography to give the sub-title compound. The catalyst was removed by filtration the mixture was concentrated The crude was purified by chromatography

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 described in step-1 of Intermediate-61 by using N-(3-amino-4-chlorobenzyl)pivalamide (1.80 g), NaNO2 (0.62 g, 0.009 mmol), SnCl2.2H2O (4.2 g, 0.018 mmol) and conc. HCl (30 mL) to afford 1.5 g of the desired product. 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 described in step-2 of Intermediate-83 by using 5-(aminomethyl)-2-chlorobenzenamine (2.0 g), pivaloyl chloride (0.2 mL), TEA (2 mL) and THF (10 mL) to afford 2.0 g of the desired product. 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 described in step-1 of Intermediate-61 by using N-(3-amino-4-chlorobenzyl)pivalamide (1.80 g), NaNO2 (0.62 g, 0.009 mmol), SnCl2.2H2O (4.2 g, 0.018 mmol) and conc. HCl (30 mL) to afford 1.5 g of the desired product. The title compound was prepared