反应详情

To a stirred solution of (4S,5S)-tert-butyl 5-((2,2-dimethylhexanamido)methyl)-4-((S)-2-(hydroxy(1-(3-methoxypropyl)-1H-indazol-6-yl)methyl)-3-methylbutyl)-2,2-dimethyloxazolidine-3-carboxylate (45 mg, 0.07 mmol) in CH2Cl2 (8 mL) at 0° C. was added TFA (2 mL). The mixture was stirred for ˜1 h and concentrated. The residue was purified by preparative HPLC to give N-((2S,3S,5S)-3-amino-2-hydroxy-5-(hydroxy(1-(3-methoxypropyl)-1H-indazol-6-yl)methyl)-6-methylheptyl)-2,2-dimethylhexanamide as its TFA salt (15 mg, 42%). 1H NMR (400 MHz, CD3OD): δ 8.00 (s, 1H), 7.74 (d, J=8.4 Hz, 1H), 7.55 (m, 1H), 7.17 (m, 1H), 4.50 (m, 2H), 3.84-3.68 (m, 2H), 3.45 (m, 1H), 3.27 (s, 3H), 3.25-3.18 (m, 3H), 2.13 (m, 2H), 1.89-1.72 (m, 2H), 1.55 (m, 3H), 1.32-1.11 (m, 9H), 0.99-0.80 (m, 12H); MS: 489 (M++1).

1. concentrationconcentrated
2. customThe residue was purified by preparative HPLC