反应详情

A solution of ((S)-5-[2-(4-benzyloxy-phenyl)-acetylamino]-1-{[(3,5-diamino-6-chloro-pyrazine-2-carbonyl)-amino]-methyl}-pentyl)-carbamic acid tert-butyl ester (0.1 g, 0.16 mmol) in DCM (3 mL) and TFA (1 mL) is stirred at RT for 6 h. The solvent is removed in vacuo and the resulting residue is dissolved in DMSO and purified by reverse phase column chromatography (Isolute™ C18, 0-100% acetonitrile in water-0.1% TFA) to afford the title compound. [M+H]+ 526. 1H NMR (500 MHz, DMSO-d6) δ 8.16 (1H, t), 8.05 (1H, t), 7.94 (4H, br), 7.42 (2H, d), 7.37 (2H, dd), 7.31 (1H, dd), 7.16 (2H, d), 7.04 (2H, br), 6.92 (2H, d), 5.05 (2H, s), 3.38 (2H, m), 3.31 (2H, s), 3.18 (1H, m), 3.02 (2H, m), 1.52 (2H, m), 1.38 (4H, m).

1. customThe solvent is removed in vacuo
2. dissolutionthe resulting residue is dissolved in DMSO
3. custompurified by reverse phase column chromatography (Isolute™ C18, 0-100% acetonitrile in water-0.1% TFA)