6-oxa-9-azaspiro[4.5]decane

反応条件: temp:70.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: 6-Bromo-4-[5-(chloromethyl)-1,3,4-oxadiazol-2-yl]-1-(phenylsulfonyl)-1H-indazole (200 mg, 0.441 mmol) in acetonitrile (2 ml) was treated with 6-oxa-9-azaspiro[4.5]decane (160 mg, 0.793 mmol), DIPEA (0.154 ml, 0.8825 mmol) and sodium iodide (66 mg, 0.44 mmol). The reaction mixture was heated at 70° C. for 5 h, then cooled, diluted with DCM and washed with aqueous HCl. The organic layer was separated using a hydrophobic frit, washed with water and the solvent removed under a stream of nitrogen. The resulting residue was purified by loading onto a silica cartridge (20 g) and eluting with 0-100% ethyl acetate/cyclohexane over 40 mins. The appropriate fractions were combined and evaporated to give the title compound as a yellow solid (74 mg). cooled washed with aqueous HCl The organic layer was separated washed with water the solvent removed under a stream of nitrogen The resulting residue was purified eluting with 0-100% ethyl acetate/cyclohexane over 40 mins evaporated

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

実験手順: To a of solution 1,1-dimethylethyl 6-oxa-9-azaspiro[4.5]decane-9-carboxylate (200 mg, 0.829 mmol, available from Tyger Scientific Inc) in DCM (3 ml) was added trifluoroacetic acid (TFA) (0.5 ml). The resulting colourless yellow solution was stirred at room temperature for 24 hr. The solvent was evaporated to give the title compound as a grey oil (203 mg). The solvent was evaporated

反応条件: temp:0.00; pressure:0.00; stir:

反応条件: temp:70.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: 6-Bromo-4-[5-(chloromethyl)-1,3,4-oxadiazol-2-yl]-1-(phenylsulfonyl)-1H-indazole (200 mg, 0.441 mmol) in acetonitrile (2 ml) was treated with 6-oxa-9-azaspiro[4.5]decane (160 mg, 0.793 mmol), DIPEA (0.154 ml, 0.8825 mmol) and sodium iodide (66 mg, 0.44 mmol). The reaction mixture was heated at 70° C. for 5 h, then cooled, diluted with DCM and washed with aqueous HCl. The organic layer was separated using a hydrophobic frit, washed with water and the solvent removed under a stream of nitrogen. The resulting residue was purified by loading onto a silica cartridge (20 g) and eluting with 0-100% ethyl acetate/cyclohexane over 40 mins. The appropriate fractions were combined and evaporated to give the title compound as a yellow solid (74 mg). cooled washed with aqueous HCl The organic layer was separated washed with water the solvent removed under a stream of nitrogen The resulting residue was purified eluting with 0-100% ethyl acetate/cyclohexane over 40 mins evaporated

反応条件: temp:70.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: 6-Bromo-4-[5-(chloromethyl)-1,3,4-oxadiazol-2-yl]-1-(phenylsulfonyl)-1H-indazole (200 mg, 0.441 mmol) in acetonitrile (2 ml) was treated with 6-oxa-9-azaspiro[4.5]decane (160 mg, 0.793 mmol), DIPEA (0.154 ml, 0.8825 mmol) and sodium iodide (66 mg, 0.44 mmol). The reaction mixture was heated at 70° C. for 5 h, then cooled, diluted with DCM and washed with aqueous HCl. The organic layer was separated using a hydrophobic frit, washed with water and the solvent removed under a stream of nitrogen. The resulting residue was purified by loading onto a silica cartridge (20 g) and eluting with 0-100% ethyl acetate/cyclohexane over 40 mins. The appropriate fractions were combined and evaporated to give the title compound as a yellow solid (74 mg). cooled washed with aqueous HCl The organic layer was separated washed with water the solvent removed under a stream of nitrogen The resulting residue was purified eluting with 0-100% ethyl acetate/cyclohexane over 40 mins evaporated

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

実験手順: To a of solution 1,1-dimethylethyl 6-oxa-9-azaspiro[4.5]decane-9-carboxylate (200 mg, 0.829 mmol, available from Tyger Scientific Inc) in DCM (3 ml) was added trifluoroacetic acid (TFA) (0.5 ml). The resulting colourless yellow solution was stirred at room temperature for 24 hr. The solvent was evaporated to give the title compound as a grey oil (203 mg). The solvent was evaporated

反応条件: temp:70.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: 6-Bromo-4-[5-(chloromethyl)-1,3,4-oxadiazol-2-yl]-1-(phenylsulfonyl)-1H-indazole (200 mg, 0.441 mmol) in acetonitrile (2 ml) was treated with 6-oxa-9-azaspiro[4.5]decane (160 mg, 0.793 mmol), DIPEA (0.154 ml, 0.8825 mmol) and sodium iodide (66 mg, 0.44 mmol). The reaction mixture was heated at 70° C. for 5 h, then cooled, diluted with DCM and washed with aqueous HCl. The organic layer was separated using a hydrophobic frit, washed with water and the solvent removed under a stream of nitrogen. The resulting residue was purified by loading onto a silica cartridge (20 g) and eluting with 0-100% ethyl acetate/cyclohexane over 40 mins. The appropriate fractions were combined and evaporated to give the title compound as a yellow solid (74 mg). cooled washed with aqueous HCl The organic layer was separated washed with water the solvent removed under a stream of nitrogen The resulting residue was purified eluting with 0-100% ethyl acetate/cyclohexane over 40 mins evaporated

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

実験手順: To a of solution 1,1-dimethylethyl 6-oxa-9-azaspiro[4.5]decane-9-carboxylate (200 mg, 0.829 mmol, available from Tyger Scientific Inc) in DCM (3 ml) was added trifluoroacetic acid (TFA) (0.5 ml). The resulting colourless yellow solution was stirred at room temperature for 24 hr. The solvent was evaporated to give the title compound as a grey oil (203 mg). The solvent was evaporated

反応条件: temp:70.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: 6-Bromo-4-[5-(chloromethyl)-1,3,4-oxadiazol-2-yl]-1-(phenylsulfonyl)-1H-indazole (200 mg, 0.441 mmol) in acetonitrile (2 ml) was treated with 6-oxa-9-azaspiro[4.5]decane (160 mg, 0.793 mmol), DIPEA (0.154 ml, 0.8825 mmol) and sodium iodide (66 mg, 0.44 mmol). The reaction mixture was heated at 70° C. for 5 h, then cooled, diluted with DCM and washed with aqueous HCl. The organic layer was separated using a hydrophobic frit, washed with water and the solvent removed under a stream of nitrogen. The resulting residue was purified by loading onto a silica cartridge (20 g) and eluting with 0-100% ethyl acetate/cyclohexane over 40 mins. The appropriate fractions were combined and evaporated to give the title compound as a yellow solid (74 mg). cooled washed with aqueous HCl The organic layer was separated washed with water the solvent removed under a stream of nitrogen The resulting residue was purified eluting with 0-100% ethyl acetate/cyclohexane over 40 mins evaporated

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

実験手順: To a of solution 1,1-dimethylethyl 6-oxa-9-azaspiro[4.5]decane-9-carboxylate (200 mg, 0.829 mmol, available from Tyger Scientific Inc) in DCM (3 ml) was added trifluoroacetic acid (TFA) (0.5 ml). The resulting colourless yellow solution was stirred at room temperature for 24 hr. The solvent was evaporated to give the title compound as a grey oil (203 mg). The solvent was evaporated

反応条件: temp:70.01; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: 6-Bromo-4-[5-(chloromethyl)-1,3,4-oxadiazol-2-yl]-1-(phenylsulfonyl)-1H-indazole (200 mg, 0.441 mmol) in acetonitrile (2 ml) was treated with 6-oxa-9-azaspiro[4.5]decane (160 mg, 0.793 mmol), DIPEA (0.154 ml, 0.8825 mmol) and sodium iodide (66 mg, 0.44 mmol). The reaction mixture was heated at 70° C. for 5 h, then cooled, diluted with DCM and washed with aqueous HCl. The organic layer was separated using a hydrophobic frit, washed with water and the solvent removed under a stream of nitrogen. The resulting residue was purified by loading onto a silica cartridge (20 g) and eluting with 0-100% ethyl acetate/cyclohexane over 40 mins. The appropriate fractions were combined and evaporated to give the title compound as a yellow solid (74 mg). cooled washed with aqueous HCl The organic layer was separated washed with water the solvent removed under a stream of nitrogen The resulting residue was purified eluting with 0-100% ethyl acetate/cyclohexane over 40 mins evaporated

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

実験手順: To a of solution 1,1-dimethylethyl 6-oxa-9-azaspiro[4.5]decane-9-carboxylate (200 mg, 0.829 mmol, available from Tyger Scientific Inc) in DCM (3 ml) was added trifluoroacetic acid (TFA) (0.5 ml). The resulting colourless yellow solution was stirred at room temperature for 24 hr. The solvent was evaporated to give the title compound as a grey oil (203 mg). The solvent was evaporated