反应详情

To a mixture of PS-isocyanate resin (2.0 g) in THF (5 mL) is added tetrabutylammonium fluoride (1.0 M in THF, 2.17 mL) and the mixture is stirred at RT for 2 h. The resin is filtered off and the filtrate is added to a solution of 5-(2-benzyloxy-4-thiazol-5-yl-phenyl)-1,1-dioxo-2-(2-trimethylsilanylethyl)-1,2,5-thiadiazolidin-3-one (272 mg, 0.543 mmol) in THF (1 mL) and the mixture is stirred at 50° C. for 18 h. The reaction mixture is cooled and diluted with EtOAc, washed with 1N HCl and dried over MgSO4. The solvent is removed under reduced pressure and the residue is purified by column chromatography eluting with MeOH/EtOAc to afford the title compound as a yellow solid: (M+1)+=402.

1. filtrationThe resin is filtered off
2. stirringthe mixture is stirred at 50° C. for 18 h
3. temperatureThe reaction mixture is cooled
4. washwashed with 1N HCl
5. dry with materialdried over MgSO4
6. customThe solvent is removed under reduced pressure
7. customthe residue is purified by column chromatography
8. washeluting with MeOH/EtOAc