反应详情

To a solution of 2-[(R)-5-(4-carbamoyl-phenyl)-indan-1-yl]-2,7-diazaspiro[3.5]nonane-7-carboxylic acid tert-butyl ester (4-1a, 124 mg, 0.27 mmol) in EtOAc (10 mL) was added 3 mL of 4N HCl in dioxane, resulting in the immediate precipitation of solids. The reaction was stirred for 3 hours. The reaction was concentrated and the residue was coevaporated with diethylether (3×) to provide 4-[(R)-1-(2,7-diaza-spiro[3.5]non-2-yl)-indan-5-yl]-benzamide hydrochloride as a white solid (102 mg, 95%). This material was used without further purification in the next reaction. MS (ES+) 362.5 (M+H)+. 1H NMR (CD3OD) δ 2.12-2.27 (m, 4H), 2.51 (dd, 1H), 2.95-3.03 (m, 1H), 3.13-3.24 (m, 4H), 3.31 (d, 3H), 4.08 (d, 1H), 4.19 (s, 2H), 4.43 (d, 1H), 5.05 (br s, 2H), 7.51-7.62 (m, 2H), 7.64-7.83 (m, 3H), 7.89-7.96 (m, 2H).

1. customresulting in the immediate precipitation of solids
2. concentrationThe reaction was concentrated