1-ethenylsulfonyl-3,3-difluoroazetidine

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: Following the procedure for 320, 8-azetidin-3-yl-2-(2-isopropyl-2H-[1,2,4]triazol-3-yl)-4,5-dihydro-6-oxa-3-thia-1-aza-benzo[e]azulene TFA salt 235 and 1-ethenesulfonyl-3,3-difluoro-azetidine were reacted to give 454 isolated as a white solid (139 mg, 84%). LCMS: RT=8.30 min, [M+H]+=551. 1H NMR δ (ppm) (CDCl3): 8.32 (1H, d, J=8.18 Hz), 7.89 (1H, s), 7.08 (1H, dd, J=8.21, 1.87 Hz), 6.97 (1H, d, J=1.84 Hz), 5.93-5.83 (1H, m), 4.38 (2H, t, J=5.05 Hz), 4.31 (4H, t, J=12.10 Hz), 3.76 (2H, t, J=6.86 Hz), 3.75-3.63 (1H, m), 3.43-3.36 (2H, m), 3.23 (2H, t, J=6.61 Hz), 3.11 (2H, t, J=7.01 Hz), 2.92 (2H, t, J=7.00 Hz), 1.60 (6H, d, J=6.63 Hz) were reacted

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 by a similar procedure to 8-(1-ethenesulfonyl-azetidin-3-yl)-2-(2-isopropyl-2H-[1,2,4]triazol-3-yl)-4,5-dihydro-6-oxa-3-thia-1-aza-benzo[e]azulene using 3,3-difluoroazetidine hydrochloride salt. 1-Ethenesulfonyl-3,3-difluoro-azetidine was isolated as a light brown oil after flash chromatography (SiO2, DCM) (171 mg, 61%). 1H NMR δ (ppm) (CDCl3): 6.56 (1H, dd, J=16.56, 9.83 Hz), 6.40 (1H, d, J=16.59 Hz), 6.20 (1H, d, J=9.83 Hz), 4.32-4.17 (4H, m)

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 by a similar procedure to 8-(1-ethenesulfonyl-azetidin-3-yl)-2-(2-isopropyl-2H-[1,2,4]triazol-3-yl)-4,5-dihydro-6-oxa-3-thia-1-aza-benzo[e]azulene using 3,3-difluoroazetidine hydrochloride salt. 1-Ethenesulfonyl-3,3-difluoro-azetidine was isolated as a light brown oil after flash chromatography (SiO2, DCM) (171 mg, 61%). 1H NMR δ (ppm) (CDCl3): 6.56 (1H, dd, J=16.56, 9.83 Hz), 6.40 (1H, d, J=16.59 Hz), 6.20 (1H, d, J=9.83 Hz), 4.32-4.17 (4H, m)

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: Following the procedure for 320, 8-azetidin-3-yl-2-(2-isopropyl-2H-[1,2,4]triazol-3-yl)-4,5-dihydro-6-oxa-3-thia-1-aza-benzo[e]azulene TFA salt 235 and 1-ethenesulfonyl-3,3-difluoro-azetidine were reacted to give 454 isolated as a white solid (139 mg, 84%). LCMS: RT=8.30 min, [M+H]+=551. 1H NMR δ (ppm) (CDCl3): 8.32 (1 H, d, J=8.18 Hz), 7.89 (1 H, s), 7.08 (1 H, dd, J=8.21, 1.87 Hz), 6.97 (1 H, d, J=1.84 Hz), 5.93-5.83 (1 H, m), 4.38 (2 H, t, J=5.05 Hz), 4.31 (4 H, t, J=12.10 Hz), 3.76 (2 H, t, J=6.86 Hz), 3.75-3.63 (1 H, m), 3.43-3.36 (2 H, m), 3.23 (2 H, t, J=6.61 Hz), 3.11 (2H, t, J=7.01 Hz), 2.92 (2 H, t, J=7.00 Hz), 1.60 (6 H, d, J=6.63 Hz) were reacted

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

実験手順: Following the procedure for 320, 8-azetidin-3-yl-2-(2-isopropyl-2H-[1,2,4]triazol-3-yl)-4,5-dihydro-6-oxa-3-thia-1-aza-benzo[e]azulene TFA salt 235 and 1-ethenesulfonyl-3,3-difluoro-azetidine were reacted to give 454 isolated as a white solid (139 mg, 84%). LCMS: RT=8.30 min, [M+H]+=551. 1H NMR δ (ppm) (CDCl3): 8.32 (1 H, d, J=8.18 Hz), 7.89 (1 H, s), 7.08 (1 H, dd, J=8.21, 1.87 Hz), 6.97 (1 H, d, J=1.84 Hz), 5.93-5.83 (1 H, m), 4.38 (2 H, t, J=5.05 Hz), 4.31 (4 H, t, J=12.10 Hz), 3.76 (2 H, t, J=6.86 Hz), 3.75-3.63 (1 H, m), 3.43-3.36 (2 H, m), 3.23 (2 H, t, J=6.61 Hz), 3.11 (2H, t, J=7.01 Hz), 2.92 (2 H, t, J=7.00 Hz), 1.60 (6 H, d, J=6.63 Hz) were reacted

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 by a similar procedure to 8-(1-ethenesulfonyl-azetidin-3-yl)-2-(2-isopropyl-2H-[1,2,4]triazol-3-yl)-4,5-dihydro-6-oxa-3-thia-1-aza-benzo[e]azulene using 3,3-difluoroazetidine hydrochloride salt. 1-Ethenesulfonyl-3,3-difluoro-azetidine was isolated as a light brown oil after flash chromatography (SiO2, DCM) (171 mg, 61%). 1H NMR δ (ppm) (CDCl3): 6.56 (1 H, dd, J=16.56, 9.83 Hz), 6.40 (1 H, d, J=16.59 Hz), 6.20 (1 H, d, J=9.83 Hz), 4.32-4.17 (4 H, m)

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

実験手順: Following the procedure for 320, 8-azetidin-3-yl-2-(2-isopropyl-2H-[1,2,4]triazol-3-yl)-4,5-dihydro-6-oxa-3-thia-1-aza-benzo[e]azulene TFA salt 235 and 1-ethenesulfonyl-3,3-difluoro-azetidine were reacted to give 454 isolated as a white solid (139 mg, 84%). LCMS: RT=8.30 min, [M+H]+=551. 1H NMR δ (ppm) (CDCl3): 8.32 (1 H, d, J=8.18 Hz), 7.89 (1 H, s), 7.08 (1 H, dd, J=8.21, 1.87 Hz), 6.97 (1 H, d, J=1.84 Hz), 5.93-5.83 (1 H, m), 4.38 (2 H, t, J=5.05 Hz), 4.31 (4 H, t, J=12.10 Hz), 3.76 (2 H, t, J=6.86 Hz), 3.75-3.63 (1 H, m), 3.43-3.36 (2 H, m), 3.23 (2 H, t, J=6.61 Hz), 3.11 (2 H, t, J=7.01 Hz), 2.92 (2 H, t, J=7.00 Hz), 1.60 (6 H, d, J=6.63 Hz) were reacted

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 by a similar procedure to 8-(1-ethenesulfonyl-azetidin-3-yl)-2-(2-isopropyl-2H-[1,2,4]triazol-3-yl)-4,5-dihydro-6-oxa-3-thia-1-aza-benzo[e]azulene using 3,3-difluoroazetidine hydrochloride salt. 1-Ethenesulfonyl-3,3-difluoro-azetidine was isolated as a light brown oil after flash chromatography (SiO2, DCM) (171 mg, 61%). 1H NMR δ (ppm) (CDCl3): 6.56 (1 H, dd, J=16.56, 9.83 Hz), 6.40 (1H, d, J=16.59 Hz), 6.20 (1 H, d, J=9.83 Hz), 4.32-4.17 (4 H, m)

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

実験手順: Following the procedure for 320, 8-azetidin-3-yl-2-(2-isopropyl-2H-[1,2,4]triazol-3-yl)-4,5-dihydro-6-oxa-3-thia-1-aza-benzo[e]azulene TFA salt 235 and 1-ethenesulfonyl-3,3-difluoro-azetidine were reacted to give 454 isolated as a white solid (139 mg, 84%). LCMS: RT=8.30 min, [M+H]+=551. 1H NMR δ (ppm) (CDCl3): 8.32 (1H, d, J=8.18 Hz), 7.89 (1H, s), 7.08 (1H, dd, J=8.21, 1.87 Hz), 6.97 (1H, d, J=1.84 Hz), 5.93-5.83 (1H, m), 4.38 (2H, t, J=5.05 Hz), 4.31 (4H, t, J=12.10 Hz), 3.76 (2H, t, J=6.86 Hz), 3.75-3.63 (1H, m), 3.43-3.36 (2H, m), 3.23 (2H, t, J=6.61 Hz), 3.11 (2H, t, J=7.01 Hz), 2.92 (2H, t, J=7.00 Hz), 1.60 (6H, d, J=6.63 Hz) were reacted

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 by a similar procedure to 8-(1-ethenesulfonyl-azetidin-3-yl)-2-(2-isopropyl-2H-[1,2,4]triazol-3-yl)-4,5-dihydro-6-oxa-3-thia-1-aza-benzo[e]azulene using 3,3-difluoroazetidine hydrochloride salt. 1-Ethenesulfonyl-3,3-difluoro-azetidine was isolated as a light brown oil after flash chromatography (SiO2, DCM) (171 mg, 61%). 1H NMR δ (ppm) (CDCl3): 6.56 (1H, dd, J=16.56, 9.83 Hz), 6.40 (1H, d, J=16.59 Hz), 6.20 (1H, d, J=9.83 Hz), 4.32-4.17 (4H, m)