With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.5908-62-3,1,1-Dioxo-isothiazolidine,as a common compound, the synthetic route is as follows.,5908-62-3
Intermediate 6 (0.090 g, 0.093 mmol) was combined with isothiazolidine 1,1-dioxide (0.112 g, 0.926 mmol) in anhydrous dichloromethane (0.93 mE). paraToluenesulfonic acid monohydrate (1.761 mg, 9.26 tmol) was added in one portion. The reaction was stirred at room temperature for 100 minutes.10510] The entire reaction mixture was purified by silica gel flash column chromatography (0-40% acetone-heptane, gradient elution, 24 g silica column, TEC in 40% acetoneheptane, visualize under UV) to give a mixture of Example 18 and residual unreacted isothiazolidine 1,1-dioxide.10511] The mixed material was again purified by silica gel flash column chromatography (0-50% acetonitrile-dichloromethane, gradient elution, 24 g column, TEC in 30% acetonitrile-dichloromethane, visualize under UV) to give Example 18 (0.02 1 g, 0.019 mmol, 20.4% yield) as a white solid.Example 1810512] ESIMS [M+NH4] 1078.9, [M-H] 1059.9.10513] HRMS: calculated for C57H92N2014SNa sodiumadduct-1083.6167. Found 1083.6151.10514] ?H NMR (600 MHz, Chloroform-d) oe 6.45 (dd,J=14.5, 11.0 Hz, 1H), 6.21 (dd, J=14.6, 10.7 Hz, 1H), 6.14(dd, J=14.8, 10.8 Hz, 1H), 5.98 (d, J=10.9 Hz, 1H), 5.35 (dd,J=14.8, 9.8 Hz, 1H), 5.20 (d, J=5.8 Hz, 1H), 5.09 (d, J=9.8Hz, 1H), 4.72 (d, J=12.1 Hz, 1H), 4.61 (m, 1H), 4.46 (s, 1H),4.10 (d, J=6.9 Hz, 1H), 3.96 (t, J=11.4 Hz, 1H), **373 (t,J=5.5 Hz, 2H), 3.68 (d, J=6.9 Hz, 1H), 3.59 (m, 4H), 3.53(m, 2H), 3.46 (s, 3H), 3.28 (s, 3H), 3.21 (m, 1H), 3.13 (m,1H), 3.07 (m, 2H), 3.05-2.99 (m, 1H), 2.97 (q, J=8.0 Hz,1H), 2.78 (dq, J=14.4, 7.1 Hz, 1H), 2.44-2.33 (m, 1H), 2.31(m, 2H), 2.27-2.19 (m, 1H), 2.19-2.12 (m, 2H), 2.07-1.94 (m, 2H), 1.88 (s, 3H), 1.83 (d, J=12.9 Hz, 1H), 1.74 (m, 3H),1.66 (m, 7H), 1.56-1.44 (m, 1H), 1.43 (m, 2H), 1.41-1.15(m, 12H), 1.04 (m, 7H), 0.91 (m, 8H), 0.84 (d, J=6.7 Hz,3H), 0.70 (q, J=12.0 Hz, 1H).
The synthetic route of 5908-62-3 has been constantly updated, and we look forward to future research findings.
Reference£º
Patent; NOVARTIS AG; BONAZZI, Simone; CONNOLLY, Michael; GLASS, David Jonathan; MIHALIC, Manuel; PATTERSON, Andrew William; ROGGO, Silvio; SHAVLAKADZE, Tea; (68 pag.)US2019/92788; (2019); A1;,
Thiazolidine – Wikipedia
Thiazolidine – ScienceDirect.com