反应详情

DIPEA (156.8 mg, 1.2 mmol) was added to a stirred solution of [(1-pyridin-3-yl-1H-[1,2,3]triazole-4-carbonyl)-amino]-acetic acid (prepared by the method used for the synthesis of Intermediate 64, starting from 3-aminopyridine, and subsequently, application of Step 3 of the General Scheme) (75 mg, 0.3 mmol) in DMF (3 mL) followed by HOBt (45 mg, 0.33 mmol) and EDCI (116 mg, 0.6 mmol). After 2 minutes of stirring, 3-(2,5-difluoro-phenoxy)-pyrrolidine hydrochloride (prepared by the method used for the synthesis of Intermediate 72) (71.5 mg, 0.3 mmol) was added and the resulting mixture was stirred at room temperature overnight. Cold water was then added and precipitate was collected to afford 48 mg (37.2% Yield) of 1-pyridin-3-yl-1H-[1,2,3]triazole-4-carboxylic acid {2-[3-(2,5-difluoro-phenoxy)-pyrrolidin-1-yl]-2-oxo-ethyl}-amide. LC/MS [M+H]+: 429.14, 92.32%. 1H NMR (300 MHz, DMSO-d6): δ 9.5 (s, 1H), 9.2 (d, 1H), 8.75 (d, 1H), 8.6 (m, 1H), 8.4 (m, 1H), 7.7 (q, 1H), 7.3-7.2 (m, 2H), 6.9-6.7 (m, 1H), 5.3-5.1 (d, 1H), 4.25-4.1 (m, 2H), 4.0-3.5 (m, 4H), 2.3-2.2 (m, 1H), 2.2-2.05 (m, 1H).

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2. additionwas added
3. stirringthe resulting mixture was stirred at room temperature overnight
4. customprecipitate was collected