反应详情

5-bromo-2-[2-(4-isopropylsulfonylphenyl)-5-trityl-pyrrolo[2,3-b]pyrazin-7-yl]isoindolin-1-one (50 mg, 0.06634 mmol) suspended in DCM (2 mL) under N2 and triethylsilane (53 μL, 0.3317 mmol) then TFA (300 μL, 3.894 mmol) added. RM stirred overnight then concentrated. Residue partitioned between DCM and saturated NaHCO3 solution. Organic phase washed with brine then dried and concentrated to a yellow solid. Dried at 60° C. in a vacuum oven to give title compound as a pale yellow solid (17 mg, 49%); 1H NMR (400 MHz, DMSO) δ1.22 (6H, d), 3.50 (1H, sep), 5.54 (2H, s), 7.77 (2H, s), 7.99 (2H, d), 8.08 (1H, s), 8.51-8.55 (3H, m), 9.11 (1H, s), 12.36 (1H, brs) ppm; MS (ES+) 512.0.

1. concentrationthen concentrated
2. customResidue partitioned between DCM and saturated NaHCO3 solution
3. washOrganic phase washed with brine
4. customthen dried
5. concentrationconcentrated to a yellow solid
6. customDried at 60° C. in a vacuum oven