反应详情

N-[(4R,4aR,6R,8aS)-8a-(2,4-difluorophenyl)-6-(ethoxymethyl)-4-methyl-4,4a,5,6,8,8a-hexahydropyrano[3,4-d][1,3]thiazin-2-yl]benzamide (C25) was deprotected using the method described for conversion of N-[(4R,4aR,6R,8aS)-8a-(2,4-difluorophenyl)-6-(methoxymethyl)-4-methyl-4,4a,5,6,8,8a-hexahydropyrano[3,4-d][1,3]thiazin-2-yl]benzamide (C20) to (4R,4aR,6R,8aS)-8a-(2,4-difluorophenyl)-6-(methoxymethyl)-4-methyl-4,4a,5,6,8,8a-hexahydropyrano[3,4-d][1,3]thiazin-2-amine (2) in Example 2. The product was obtained as a white solid. Yield: 15.0 mg, 42.1 μmol, 79%. LCMS m/z 357.2 [M+H+]. 1H NMR (400 MHz, CD3OD) δ 7.32 (ddd, J=9, 9, 7 Hz, 1H), 6.92-7.01 (m, 2H), 4.11 (dd, J=11.1, 2.0 Hz, 1H), 3.74-3.82 (m, 1H), 3.73 (d, J=11.1 Hz, 1H), 3.48-3.60 (m, 3H), 3.45 (dd, half of ABX pattern, J=10.4, 4.0 Hz, 1H), 3.06-3.14 (m, 1H), 2.75 (ddd, J=12.1, 3.9, 3.7 Hz, 1H), 1.57-1.64 (m, 1H), 1.36-1.47 (m, 1H), 1.15-1.22 (m, 6H).

1. customThe product was obtained as a white solid