Hydrochloric Acid → HCID 67406275, compound

Participants

Reaction Steps

To a mixture of 2-[(R)-5-(6-carbamoyl-pyridin-3-yl)-indan-1-yl]-2,7-diaza-spiro[3.5]nonane-7-carboxylic acid tert-butyl ester (9-1a, 440 mg, 0.95 mmol) in 1,4-dioxane (10 mL) was added 5 mL of 4N HCl in dioxane. This resulted 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×) until 5-[(R)-1-(2,7-diaza-spiro[3.5]non-2-yl)-indan-5-yl]-pyridine-2-carboxylic acid amide dihydrochloride (9-1b, 414 mg, 100%) was obtained as a white solid. This material was used without further purification in the next reaction. MS (ES+) 363.1 (M+H)+. 1H NMR (CD3OD) δ 2.22-2.26 (m, 5H), 2.56-2.66 (m, 1H), 3.19-3.22 (m, 4H), 3.35 (s, 1H), 3.63-3.66 (m, 1H), 4.15 (d, 1H), 4.24 (s, 2H), 4.47 (s, 1H), 5.09 (br s, 1H), 7.85 (s, 1H), 7.81 (s, 2H), 8.29-8.31 (m, 3H), 8.45 (br s, 1H), 9.07 (br s, 1H).

Provenance & Evidence