Sulfamide, N-3-oxetanyl- synthesis

Yield:-

Reaction Conditions:

with SULFAMIDE in water at 70 - 100; for 32 h;

Steps:

33

Intermediate 33 :3- Sulfamoylamino)oxetaneSulfamide (15.6 mmol) was dissolved in H₂0 (8 mL), added oxetan-3-amine (6.85 mmol) and stirred at 70°C for 16h and then at 100°C for another 16h. The obtained reaction mixture was cooled to rt and freezedried affording the title compound as white solid. Used without further purification. 1H NMR (300 MHz, DMSO) δ 7.44 (d, J = 8.0 Hz, 1H), 6.64 (s, 2H), 4.77 - 4.58 (m, 2H), 4.49 (t, J = 6.2 Hz, 2H), 4.45 - 4.33 (m, 1H).

References:

WO2012/93169,2012,A1 Location in patent:Page/Page column 81