morpholin-2-ylmethanamine

反応条件: temp:22.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: To a stirred solution of morpholin-2-ylmethylamine (3.1 g) in methanol (70 ml) under nitrogen was added an ethereal solution of ethyl-α,α,α-trifluoroacetate (5 ml in 20 ml ether) which had been washed with saturated aqueous sodium bicarbonate, water and brine, and dried. The mixture was stirred for 30 min at 22° C. before removal of all volatiles in vacuo. The residue was dissolved in methanol (10 ml) and the volatiles again removed in vacuo to give the title compound as a white crunchy foam (4.9 g). had been washed with saturated aqueous sodium bicarbonate, water and brine dried The residue was dissolved in methanol (10 ml) the volatiles again removed in vacuo

反応条件: temp:22.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: To a stirred solution of morpholin-2-ylmethylamine (3.1 g) in methanol (70 ml) under nitrogen was added an ethereal solution of ethyl-α,α,α-trifluoroacetate (5 ml in 20 ml ether) which had been washed with saturated aqueous sodium bicarbonate, water and brine, and dried. The mixture was stirred for 30 min at 22° C. before removal of all volatiles in vacuo. The residue was dissolved in methanol (10 ml) and the volatiles again removed in vacuo to give the title compound as a white crunchy foam (4.9 g). had been washed with saturated aqueous sodium bicarbonate, water and brine dried The residue was dissolved in methanol (10 ml) the volatiles again removed in vacuo

反応条件: temp:22.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: To a stirred solution of morpholin-2-ylmethylamine (3.1 g) in methanol (70 ml) under nitrogen was added an ethereal solution of ethyl-α,α,α-trifluoroacetate (5 ml in 20 ml ether) which had been washed with saturated aqueous sodium bicarbonate, water and brine, and dried. The mixture was stirred for 30 min at 22° C. before removal of all volatiles in vacuo. The residue was dissolved in methanol (10 ml) and the volatiles again removed in vacuo to give the title compound as a white crunchy foam (4.9 g). had been washed with saturated aqueous sodium bicarbonate, water and brine dried The residue was dissolved in methanol (10 ml) the volatiles again removed in vacuo

反応条件: temp:22.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: To a stirred solution of morpholin-2-ylmethylamine (3.1 g) in methanol (70 ml) under nitrogen was added an ethereal solution of ethyl-α,α,α-trifluoroacetate (5 ml in 20 ml ether) which had been washed with saturated aqueous sodium bicarbonate, water and brine, and dried. The mixture was stirred for 30 min at 22° C. before removal of all volatiles in vacuo. The residue was dissolved in methanol (10 ml) and the volatiles again removed in vacuo to give the title compound as a white crunchy foam (4.9 g). had been washed with saturated aqueous sodium bicarbonate, water and brine dried The residue was dissolved in methanol (10 ml) the volatiles again removed in vacuo

反応条件: temp:22.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: To a stirred solution of morpholin-2-ylmethylamine (3.1 g) in methanol (70 ml) under nitrogen was added an ethereal solution of ethyl-α,α,α-trifluoroacetate (5 ml in 20 ml ether) which had been washed with saturated aqueous sodium bicarbonate, water and brine, and dried. The mixture was stirred for 30 min at 22° C. before removal of all volatiles in vacuo. The residue was dissolved in methanol (10 ml) and the volatiles again removed in vacuo to give the title compound as a white crunchy foam (4.9 g). had been washed with saturated aqueous sodium bicarbonate, water and brine dried The residue was dissolved in methanol (10 ml) the volatiles again removed in vacuo

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

実験手順: A solution of 4-(4-hydroxy-piperidin-1-yl)-benzenesulfonic acid 2-[(4-hydroxy-piperidine-1-carbonyl)-amino]-1H-benzoimidazol-5-yl ester (example 79, 20 mg) and 2-(aminomethyl)-morpholine (50 mg) in tetrahydrofuran (1 ml) and N-methylpyrrolidinone (0.2 ml) was heated at 95° C. for 22 hours. The reaction mixture was then evaporated and purified by triggered LC/MS to give 4-(4-hydroxy-piperidin-1-yl)-benzenesulfonic acid 2-[3-(2-morpholin-4-yl-ethyl)-ureido]-1H-benzoimidazol-5-yl ester as an off-white solid (7 mg). Mass spectrum: 545 [M+H]+; retention time=5.47 minutes. The reaction mixture was then evaporated purified by triggered LC/MS

反応条件: temp:22.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: To a stirred solution of morpholin-2-ylmethylamine (3.1 g) in methanol (70 ml) under nitrogen was added an ethereal solution of ethyl-α,α,α-trifluoroacetate (5 ml in 20 ml ether) which had been washed with saturated aqueous sodium bicarbonate, water and brine, and dried. The mixture was stirred for 30 min at 22° C. before removal of all volatiles in vacuo. The residue was dissolved in methanol (10 ml) and the volatiles again removed in vacuo to give the title compound as a white crunchy foam (4.9 g). had been washed with saturated aqueous sodium bicarbonate, water and brine dried The residue was dissolved in methanol (10 ml) the volatiles again removed in vacuo

反応条件: temp:22.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: To a stirred solution of morpholin-2-ylmethylamine (3.1 g) in methanol (70 ml) under nitrogen was added an ethereal solution of ethyl-α,α,α-trifluoroacetate (5 ml in 20 ml ether) which had been washed with saturated aqueous sodium bicarbonate, water and brine, and dried. The mixture was stirred for 30 min at 22° C. before removal of all volatiles in vacuo. The residue was dissolved in methanol (10 ml) and the volatiles again removed in vacuo to give the title compound as a white crunchy foam (4.9 g). had been washed with saturated aqueous sodium bicarbonate, water and brine dried The residue was dissolved in methanol (10 ml) the volatiles again removed in vacuo

反応条件: temp:22.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: To a stirred solution of morpholin-2-ylmethylamine (3.1 g) in methanol (70 ml) under nitrogen was added an ethereal solution of ethyl-α,α,α-trifluoroacetate (5 ml in 20 ml ether) which had been washed with saturated aqueous sodium bicarbonate, water and brine, and dried. The mixture was stirred for 30 min at 22° C. before removal of all volatiles in vacuo. The residue was dissolved in methanol (10 ml) and the volatiles again removed in vacuo to give the title compound as a white crunchy foam (4.9 g). had been washed with saturated aqueous sodium bicarbonate, water and brine dried The residue was dissolved in methanol (10 ml) the volatiles again removed in vacuo

反応条件: temp:22.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: To a stirred solution of morpholin-2-ylmethylamine (3.1 g) in methanol (70 ml) under nitrogen was added an ethereal solution of ethyl-α,α,α-trifluoroacetate (5 ml in 20 ml ether) which had been washed with saturated aqueous sodium bicarbonate, water and brine, and dried. The mixture was stirred for 30 min at 22° C. before removal of all volatiles in vacuo. The residue was dissolved in methanol (10 ml) and the volatiles again removed in vacuo to give the title compound as a white crunchy foam (4.9 g). had been washed with saturated aqueous sodium bicarbonate, water and brine dried The residue was dissolved in methanol (10 ml) the volatiles again removed in vacuo