213990-48-8

860354-53-6

213990-48-8

Under nitrogen protection, benzyl (3S)-3-[(tert-butoxycarbonyl)amino]azepane-1-carboxylate (17.4 g, 50 mmol) was dissolved in methanol (200 mL), followed by careful addition of palladium hydroxide (Pd(OH)2). A hydrogen gas balloon was introduced into the reaction system and the reaction mixture was stirred overnight at room temperature. Upon completion of the reaction, the reaction mixture was filtered through a diatomaceous earth pad and the filtrate was concentrated under reduced pressure to afford tert-butyl (S)-azepane-3-carbamate (10.5 g, 98% yield), which can be used in the next step of the reaction without further purification. The product was characterized as follows: 1H NMR (d6-DMSO) δ: 6.61 (d, 1H), 3.41 (m, 2H), 2.83 (m, 1H), 2.69 (m, 1H), 2.46 (m, 1H), 1.68 (m, 2H), 1.54 (m, 2H), 1.44 (m, 2H), 1.38 (m, 1H), 1.37 (s , 9H).LCMS (APCI): m/z = 215 [M+H]+.