反应详情

A solution of [4-(4-benzyloxycarbonylaminobutyl)phenoxy]acetic acid ethyl ester 480 (0.3 g, 0.78 mmol), 2-(2-hydroxyethylamino)ethanol (0.15 m-L, 1.6 mmol), and ethanol (20 mL) was heated at 70° C. for 72 hours. The solvent was evaporated in vacuo. The residue was purified by flash chromatography (silica gel, dichloromethane/methanol, 100:5-1, v/v) to provide 490 (0.19 g, 100% based on the recovered starting material (0.13 g)) as a pale yellow solid. 1H NMR (300 MHz, CDCl3) δ 1.55 (m, 4H), 2.56 (t, 2H), 3.20 (q, 2H), 3.60 (m, 4H), 3.90 (m, 2H), 3.96 (m, 2H), 4.85 (s, 2H), 5.09 (s, 2H), 6.85 (d, 2H), 7.06 (d, 2H), 7.40 (m, 5H). m/z (ESI) 445.

1. customThe solvent was evaporated in vacuo
2. customThe residue was purified by flash chromatography (silica gel, dichloromethane/methanol, 100:5-1