反应详情

A mixture of the solid containing 3-(carboxycarbonyl)-4-methoxy-1H-pyrrolo[2,3-b]pyridine 7-oxide from above (200 mg, 0.84 mmol), triethylamine (0.5 mL, sssss), 1-(1-phenyl-1H-tetrazol-5-yl)piperazine (234 mg, 1.01 mmol) and TBTU (404 mg, 1.26 mmol) was stirred at rt in DMF (1 mL) for 24 h. H2O was added and the reaction mixture was concentrated under reduced pressure. The residue was purified using reverse phase prep HPLC to afford the title compound as a white solid (15 mg, 4%). 1H NMR (500 MHz, CDCl3) δ ppm 3.32 (s, 2H) 3.37 (s, 2H) 3.56 (s, 2H) 3.79 (s, 2H) 4.13 (s, 3H) 6.83 (d, J=7.32 Hz, 1H) 7.53 (d, J=6.71 Hz, 1H) 7.54-7.60 (m, 3H) 8.16 (s, 1H) 8.34 (d, J=6.71 Hz, 1H). LCMS: m/e 449 (M+H)+, ret time 0.99 min (method 2).

1. additionA mixture of the solid
2. concentrationthe reaction mixture was concentrated under reduced pressure
3. customThe residue was purified