Hydrochloric Acid → (S)-1-(6-(6-Methoxy-6-methyl-1,4-diazepan-1-yl)pyridin-2-yl)-6-(1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl)-1H-pyrazolo[4,3-c]pyridine

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Reaction Steps

To a solution of (R)-tert-butyl 6-methoxy-6-methyl-4-(6-(6-(1-(2,2,2-trifluoroethyl)-1H-pyrazol-4-yl)-1H-pyrazolo[4,3-c]pyridin-1-yl)pyridin-2-yl)-1,4-diazepane-1-carboxylate (100 mg, 0.17 mmol) in MeOH (5 mL) was added HCl (conc., 5 mL). The mixture was stirred at room temperature for 4 hours. It was concentrated under reduced pressure. The crude was purified by reverse phase preparative HPLC to afford 261 as a white solid (75 mg, 91%). 1H NMR (500 MHz, DMSO-d6) δ (ppm) 9.16 (s, 1H), 8.70 (s, 1H), 8.55 (s, 1H), 8.41 (s, 1H), 8.14 (s, 1H), 7.68 (t, 1H), 7.16 (d, 1H), 6.69 (d, 1H), 5.27-5.22 (m, 2H), 4.06-4.03 (m, 2H), 3.67-3.54 (m, 2H), 3.12 (s, 3H), 3.02 (s, 2H), 2.72 (s, 2H), 1.14 (s, 3H); MS (ESI) m/z: 487 [M+H]+.

Provenance & Evidence