Potassium Carbonate → 6-tert-Butyl-8-fluoro-2-(2-hydroxymethyl-3-{6-[5-(morpholine-4-carbonyl)-pyridin-2-ylamino]-pyridazin-4-yl}-phenyl)-2H-phthalazin-1-one

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Reaction Steps

Acetic acid 2-(6-tert-butyl-8-fluoro-1-oxo-1H-phthalazin-2-yl)-6-{6-[5-(morpholine-4-carbonyl)-pyridin-2-ylamino]-pyridazin-4-yl}-benzyl ester (240 mg, 0.37 mmol) was dissolved in methanol (10 ml). K2CO3 (102 mg, 0.74 mmol) was added at room temperature and the mixture was stirred at that temperature for 2 hours. After the completion of the reaction, the mixture was filtered. The filtrate was washed with water, dried over sodium sulfate and concentrated. The desired product was obtained as a yellow solid (150 mg, yield 67%). 1H NMR (300 MHz, DMSO): δ 10.56 (s, 1H), 8.96 (d, J=1.9 Hz, 1H), 8.55-8.51 (m, 1H), 8.34 (d, J=2.2 Hz, 1H), 8.23 (d, J=1.9 Hz, 1H), 7.88 (d, J=1.6 Hz, 1H), 7.85-7.73 (m, 3H), 7.65-7.47 (m, 3H), 4.88-4.80 (m, 1H), 4.28 (ddd, J=4.3, 3.1, 2.0 Hz, 2H), 3.65-3.46 (m, 8H), 1.38 (s, 9H). LC-MS: 610[M+1]+, tR=1.389 min. HPLC: 97.93% at 214 nm, 98.77% at 254 nm, tR=3.532 min.

Provenance & Evidence