Methanol → 1-(5'-Chloro-3'-fluoro-3,5-dimethyl-2,4'-bipyridin-2'-yl)piperidin-4-amine

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Reaction Steps

A solution of tert-butyl (1-(5′-chloro-3′-fluoro-3,5-dimethyl-[2,4′-bipyridin]-2′-yl)piperidin-4-yl)carbamate (160 mg, 0.368 mmol) in 4 M HCl in dioxane (3.0 mL, 12.0 mmol) and MeOH (1.0 mL) was stirred at rt for 2 h. After concentration, the residue was further dried under vacuum to give 150 mg (100%) of pale yellow solid as a di-HCl salt: LRMS (M+H)+: 335.0; 1H NMR (400 MHz, DMSO-d6) δ 1.50-1.72 (m, 2 H), 1.94-2.03 (m, 2 H), 2.10 (s, 3 H), 2.37 (s, 3 H), 2.89-3.12 (m, 2 H), 3.20-3.33 (m, 1 H), 3.92-4.08 (m, 2 H), 6.62 (br. s., 1 H), 7.77 (s, 1 H), 8.12-8.31 (m, 4 H), 8.44 (s, 1 H).

Provenance & Evidence