反应详情

2-(4-Fluoro-phenyl)-5-iodo-6-methanesulfonylamino-furo[2,3-b]pyridine-3-carboxylic acid methylamide (150 mg, 0.31 mmol) is dissolved in DMA (4 mL) and Cs2CO3 (110 mg, 0.34 mmol) and N-Allyl-N-(2-bromo-ethyl)-2-nitro-benzenesulfonamide (214 mg, 0.61 mmol) is added and the mixture is placed in the microwave for 30 min at 150° C. The mixture is then filtered and the solid is washed with EtOAc (30 mL). The organic is washed with H2O (10 mL) then Brine (20 mL) and then dried over Na2SO4 then concentrated to dryness. HPLC (CH3CN/H2O/0.1% TFA) provides 6-({2-[Allyl-(2-nitro-benzenesulfonyl)-amino]-ethyl}-methanesulfonyl-amino)-2-(4-fluoro-phenyl)-5-iodo-furo[2,3-b]pyridine-3-carboxylic acid methylamide (45 mg, 19%). MS-ES [M+H]+=758.3.

1. filtrationThe mixture is then filtered
2. washthe solid is washed with EtOAc (30 mL)
3. washThe organic is washed with H2O (10 mL)
4. dry with materialBrine (20 mL) and then dried over Na2SO4
5. concentrationthen concentrated to dryness