2,4-difluorobenzenesulfonamide

反応条件: temp:0.00; pressure:0.00; stir:

反応条件: temp:120.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: To a solution of 2,4-difluorobenzenesulfonamide (1.56 g) and 1-((4′-chlorobiphenyl-2-yl)methyl)piperazine (2.32 g) in dimethylsulfoxide (20 mL) was added N,N-diisopropylethylamine (5 mL). The mixture was stirred at 120° C. overnight. The mixture was diluted with ethyl acetate (300 mL) and washed with water (3×) brine and dried over Na2SO4. After filtration and evaporation of the solvent, the residue was loaded on a column and eluted with 40% ethyl acetate in hexane to give the title compound. washed with water (3×) brine dried over Na2SO4 After filtration and evaporation of the solvent eluted with 40% ethyl acetate in hexane

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 Example 42 from phenyl 2-(4-{4-[3-(aminocarbonyl)phenyl]-3,5-dimethyl-1H-pyrazol-1-yl}phenyl)ethylcarbamate (step 6 of example 72) and 2,4-difluorobenzensulfonamide: MS (ESI) m/z 554 [M+H]+, 552 [M−H]−, 1H-NMR (CDCl3) δ 8.00-7.98 (1H, m), 7.83-7.73 (3H, m), 7.56-7.44 (2H, m), 7.22 (4H, s), 7.05-6.94 (1H, m), 6.20 (1H, br.s), 5.66 (1H, br.s), 3.47 (2H, t, J=6.2 Hz), 2.85 (2H, t, J=6.2 Hz), 2.21 (3H, s), 2.20 (3H, s).

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 Example 42 from phenyl 2-(4-{4-[3-(aminocarbonyl)phenyl]-3,5-dimethyl-1H-pyrazol-1-yl}phenyl)ethylcarbamate (step 6 of example 72) and 2,4-difluorobenzensulfonamide: MS (ESI) m/z 554 [M+H]+, 552 [M−H]−, 1H-NMR (CDCl3) δ 8.00-7.98 (1H, m), 7.83-7.73 (3H, m), 7.56-7.44 (2H, m), 7.22 (4H, s), 7.05-6.94 (1H, m), 6.20 (1H, br.s), 5.66 (1H, br.s), 3.47 (2H, t, J=6.2 Hz), 2.85 (2H, t, J=6.2 Hz), 2.21 (3H, s), 2.20 (3H, s).

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 Example 42 from phenyl 2-[4-(3,5-dimethyl-4-phenyl-1H-pyrazol-1-yl)phenyl]ethylcarbamate (step 1 of Example 22) and 2,4-difluorobenzenesulfonamide: 1H-NMR (CDCl3) δ 7.98-7.90 (1H, m), 7.47-7.41 (2H, m), 7.35-7.22 (7H, m), 7.07-6.92 (2H, m), 6.16 (1H, br.s), 3.50-3.43 (2H, m), 2.84 (2H, t, J=6.6 Hz), 2.33 (3H, s), 2.23 (3H, s).

反応条件: temp:120.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: To a solution of 2,4-difluorobenzenesulfonamide (1.56 g) and 1-((4′-chlorobiphenyl-2-yl)methyl)piperazine (2.32 g) in dimethylsulfoxide (20 mL) was added N,N-diisopropylethylamine (5 mL). The mixture was stirred at 120° C. overnight. The mixture was diluted with ethyl acetate (300 mL) and washed with water (3×) brine and dried over Na2SO4. After filtration and evaporation of the solvent, the residue was loaded on a column and eluted with 40% ethyl acetate in hexane to give the title compound. washed with water (3×) brine dried over Na2SO4 After filtration and evaporation of the solvent eluted with 40% ethyl acetate in hexane

反応条件: temp:120.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: To a solution of 2,4-difluorobenzenesulfonamide (1.56 g) and 1-((4′-chlorobiphenyl-2-yl)methyl)piperazine (2.32 g) in dimethylsulfoxide (20 mL) was added N,N-diisopropylethylamine (5 mL). The mixture was stirred at 120° C. overnight. The mixture was diluted with ethyl acetate (300 mL) and washed with water (3×) brine and dried over Na2SO4. After filtration and evaporation of the solvent, the residue was loaded on a column and eluted with 40% ethyl acetate in hexane to give the title compound. washed with water (3×) brine dried over Na2SO4 After filtration and evaporation of the solvent eluted with 40% ethyl acetate in hexane

反応条件: temp:120.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: To a solution of 2,4-difluorobenzenesulfonamide (1.56 g) and 1-((4′-chlorobiphenyl-2-yl)methyl)piperazine (2.32 g) in dimethylsulfoxide (20 mL) was added N,N-diisopropylethylamine (5 mL). The mixture was stirred at 120° C. overnight. The mixture was diluted with ethyl acetate (300 mL) and washed with water (3×) brine and dried over Na2SO4. After filtration and evaporation of the solvent, the residue was loaded on a column and eluted with 40% ethyl acetate in hexane to give the title compound. washed with water (3×) brine dried over Na2SO4 After filtration and evaporation of the solvent eluted with 40% ethyl acetate in hexane

反応条件: temp:120.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: To a solution of 2,4-difluorobenzenesulfonamide (1.56 g) and 1-((4′-chlorobiphenyl-2-yl)methyl)piperazine (2.32 g) in dimethylsulfoxide (20 mL) was added N,N-diisopropylethylamine (5 mL). The mixture was stirred at 120° C. overnight. The mixture was diluted with ethyl acetate (300 mL) and washed with water (3×) brine and dried over Na2SO4. After filtration and evaporation of the solvent, the residue was loaded on a column and eluted with 40% ethyl acetate in hexane to give the title compound. washed with water (3×) brine dried over Na2SO4 After filtration and evaporation of the solvent eluted with 40% ethyl acetate in hexane

反応条件: temp:0.00; pressure:0.00; stir:

反応条件: temp:120.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: To a solution of 2,4-difluorobenzenesulfonamide (1.56 g) and 1-((4′-chlorobiphenyl-2-yl)methyl)piperazine (2.32 g) in dimethylsulfoxide (20 mL) was added N,N-diisopropylethylamine (5 mL). The mixture was stirred at 120° C. overnight. The mixture was diluted with ethyl acetate (300 mL) and washed with water (3×) brine and dried over Na2SO4. After filtration and evaporation of the solvent, the residue was loaded on a column and eluted with 40% ethyl acetate in hexane to give the title compound. washed with water (3×) brine dried over Na2SO4 After filtration and evaporation of the solvent eluted with 40% ethyl acetate in hexane

反応条件: temp:120.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: To a solution of 2,4-difluorobenzenesulfonamide (1.56 g) and 1-((4′-chlorobiphenyl-2-yl)methyl)piperazine (2.32 g) in dimethylsulfoxide (20 mL) was added N,N-diisopropylethylamine (5 mL). The mixture was stirred at 120° C. overnight. The mixture was diluted with ethyl acetate (300 mL) and washed with water (3×) brine and dried over Na2SO4. After filtration and evaporation of the solvent, the residue was loaded on a column and eluted with 40% ethyl acetate in hexane to give the title compound. washed with water (3×) brine dried over Na2SO4 After filtration and evaporation of the solvent eluted with 40% ethyl acetate in hexane