反应详情

A solution of (R)-2-(4-chloro-2-(2,4-dimethoxybenzyl)-7-fluoro-3-oxo-2,3-dihydro-1H-pyrrolo[3,4-c]pyridin-6-ylamino)-4-methylpentanamide (150 mg, 0.323 mmol), tributyl(furan-2-yl)stannane (138 mg, 0.387 mmol), and tetrakis(triphenylphosphine)palladium(0) (373 mg, 0.323 mmol) in toluene (1 mL) was heated to 102° C. overnight. After removal of the solvent, the residue was diluted in MeOH/DCM (10 mL) and was purified via preparative HPLC eluting with water (0.05% TFA) and ACN (45-60% gradient, 0.035% TFA). The collected fractions were stripped to dryness via rotary evaporation to give the title compound (93.1 mg, 58%). [M+H] calc'd for C26H29FN4O5, 498; found 498.

1. customAfter removal of the solvent
2. additionthe residue was diluted in MeOH/DCM (10 mL)
3. customwas purified via preparative HPLC
4. washeluting with water (0.05% TFA) and ACN (45-60% gradient, 0.035% TFA)
5. customThe collected fractions were stripped to dryness via rotary evaporation