1,4-Dioxane → (3S)-1-[3-methyl-6-[6-(6-methylpyrazin-2-yl)pyrazolo[4,3-c]pyridin-1-yl]pyrazin-2-yl]piperidin-3-amine

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A solution of tert-butyl N-[(3S)-1-[3-methyl-6-[6-(6-methylpyrazin-2-yl)pyrazolo[4,3-c]pyridin-1-yl]pyrazin-2-yl]-3-piperidyl]carbamate (34 mg, 0.068 mmol) in hydrogen chloride (4 mol/l) in 1,4-dioxane (2.0 ml, 8.0 mmol) and 1,4-dioxane 2.0 mL was stirred at RT 18 h. The crude product was submitted for reverse phase HPLC to give 228 (15 mg, 56% yield). MS (ESI) m/z: 402.2. 1H NMR (400 MHz, DMSO) δ 9.58 (s, 1H), 9.44 (s, 1H), 9.32 (s, 1H), 8.71 (s, 1H), 8.66 (s, 1H), 8.63 (s, 1H), 3.67 (d, J=12.3 Hz, 2H), 3.19 (t, J=11.3 Hz, 1H), 2.93 (s, 1H), 2.73 (dd, J=12.1, 9.1 Hz, 1H), 2.64 (s, 3H), 2.54 (s, 3H), 1.94 (d, J=10.2 Hz, 2H), 1.74 (d, J=11.1 Hz, 1H), 1.39-1.26 (m, 1H).

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