反应详情

To a solution of 2-[(R)-5-(4-methyl-pyrazol-1-yl)-indan-1-yl]-2,7-diaza-spiro[3.5]nonane-7-carboxylic acid tert-butyl ester (8-1a, 239 mg, 0.57 mmol) in MeOH (5 mL) was added 9 mL of 4N HCl in dioxane solution. The reaction was stirred for 3 hours. The reaction was concentrated and the residue was coevaporated with diethylether (3×) to afford 2-((R)-5-(4-methyl-1H-pyrazol-1-yl)-2,3-dihydro-1H-inden-1-yl)-2,7-diazaspiro[3.5]nonane dihydrochloride as a white solid (8-1b, 135 mg, 61%). This material was used without further purification in the next reaction. MS (ES+) 322.9 (M+H)+. 1H NMR (DMSO-d6) δ 1.89-2.20 (m, 7H), 2.28-2.48 (m, 2H), 2.84-3.14 (m, 4H), 3.28-3.46 (m, 1H), 3.84-4.03 (m, 3H), 4.19-4.33 (m, 2H), 4.83-4.98 (m, 1H), 7.54 (s, 1H), 7.66 (s, 2H), 7.74-7.79 (m, 1H), 8.28 (s, 1H).

1. concentrationThe reaction was concentrated