反应详情

A solution of 2-(4-cyclobutyl-[1,4]diazepane-1-carbonyl)-2-(3-fluoro-benzyl)-pyrrolidine-1-carboxylic acid tert-butyl ester (40.0 mg) in EtOH (5.0 mL) and 4 M HCl in dioxane (2.0 mL) was stirred for 10 h. The mixture was concentrated and the residue diluted with CH2Cl2 and treated with Et3N. The mixture was washed with water and concentrated to yield title compound (17 mg, 54%). MS (ESI): mass calcd. for C26H38FN3O3, 359.60; m/z found, 360.3 [M+H]+. 1H NMR (CDCl3): 7.23-6.84 (m, 4H), 3.87-3.40 (m, 4H), 3.15-3.0 (m, 1H), 2.97-2.71 (m, 4H), 2.68-2.40 (m, 4H), 2.10-1.98 (m, 3H), 1.93-1.54 (m, 9H).

1. concentrationThe mixture was concentrated
2. additionthe residue diluted with CH2Cl2
3. additiontreated with Et3N
4. washThe mixture was washed with water
5. concentrationconcentrated