2-piperidin-4-yl-1,2-thiazolidine 1,1-dioxide

反応条件: temp:0.00; pressure:0.00; stir:

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

実験手順: To the acetonitrile solution (3 mL) containing 4-(1,1-dioxo-1λ6-isothiazolidin-2-yl)piperidine (136 mg) were added 1-(4-methoxyphenylsulfonyl)-2-chloro-5-phenylbenzimidazole (340 mg) and diisopropylethylamine (0.41 mL), followed by stirring at room temperature for 16 hrs. The reaction mixture was diluted with ethyl acetate and water, and the organic layer was washed with an aqueous saturated sodium chloride solution, dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was separated and purified on a collective thin-layer chromatograph (ethyl acetate) to give the title compound (157 mg). the organic layer was washed with an aqueous saturated sodium chloride solution dried over anhydrous sodium sulfate concentrated under reduced pressure The residue was separated purified on a collective thin-layer chromatograph (ethyl acetate)

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

実験手順: 20% Palladium hydroxide (100 mg) was added to the methanol solution (5 mL) containing 4-(1,1-dioxo-1λ6-isothiazolidin-2-yl)-1-benzylpiperidine (252 mg) at 0° C., followed by stirring at room temperature for 5 hrs. under a hydrogen atmosphere. The reaction mixture was filtered to remove the palladium catalyst, followed by concentration under reduced pressure to give the title compound. The reaction mixture was filtered to remove the palladium catalyst followed by concentration under reduced pressure

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

実験手順: 20% Palladium hydroxide (100 mg) was added to the methanol solution (5 mL) containing 4-(1,1-dioxo-1λ6-isothiazolidin-2-yl)-1-benzylpiperidine (252 mg) at 0° C., followed by stirring at room temperature for 5 hrs. under a hydrogen atmosphere. The reaction mixture was filtered to remove the palladium catalyst, followed by concentration under reduced pressure to give the title compound. The reaction mixture was filtered to remove the palladium catalyst followed by concentration under reduced pressure

反応条件: temp:0.00; pressure:0.00; stir:

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

実験手順: To the acetonitrile solution (3 mL) containing 4-(1,1-dioxo-1λ6-isothiazolidin-2-yl)piperidine (136 mg) were added 1-(4-methoxyphenylsulfonyl)-2-chloro-5-phenylbenzimidazole (340 mg) and diisopropylethylamine (0.41 mL), followed by stirring at room temperature for 16 hrs. The reaction mixture was diluted with ethyl acetate and water, and the organic layer was washed with an aqueous saturated sodium chloride solution, dried over anhydrous sodium sulfate and concentrated under reduced pressure. The residue was separated and purified on a collective thin-layer chromatograph (ethyl acetate) to give the title compound (157 mg). the organic layer was washed with an aqueous saturated sodium chloride solution dried over anhydrous sodium sulfate concentrated under reduced pressure The residue was separated purified on a collective thin-layer chromatograph (ethyl acetate)

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

実験手順: 20% Palladium hydroxide (100 mg) was added to the methanol solution (5 mL) containing 4-(1,1-dioxo-1λ6-isothiazolidin-2-yl)-1-benzylpiperidine (252 mg) at 0° C., followed by stirring at room temperature for 5 hrs. under a hydrogen atmosphere. The reaction mixture was filtered to remove the palladium catalyst, followed by concentration under reduced pressure to give the title compound. The reaction mixture was filtered to remove the palladium catalyst followed by concentration under reduced pressure