Trifluoroacetic acid → HCID 86650181、化合物
反応式
C(OC([N:8]1[CH:13]2[CH2:14][CH2:15][CH:9]1[CH2:10][N:11]([C:16](=[O:21])[C:17]([F:20])([F:19])[F:18])[CH2:12]2)=O)(C)(C)C.[C:22]([OH:28])([C:24]([F:27])([F:26])[F:25])=[O:23]>C(Cl)Cl>[F:25][C:24]([F:27])([F:26])[C:22]([OH:28])=[O:23].[CH:13]12[NH:8][CH:9]([CH2:15][CH2:14]1)[CH2:10][N:11]([C:16](=[O:21])[C:17]([F:18])([F:19])[F:20])[CH2:12]2参加物
4
実験手順
To a solution of 3,8-diaza-bicyclo[3.2.1]octane-8-carboxylic acid tert-butyl ester (212 mg, 1.0 mmol) in DCM (4 mL) were added triethylamine (208 μL, 1.5 mmol) and trifluoroacetic anhydride (169 μL, 1.2 mmol) at 0° C. and the mixture stirred at 0° C. for 2 h. The reaction mixture was concentrated in vacuo and the resultant residue was purified by column chromatography to give 3-(2,2,2-trifluoro-acetyl)-3,8-diaza-bicyclo[3.2.1]octane-8-carboxylic acid tert-butyl ester as a colourless oil. To a solution of 3-(2,2,2-trifluoro-acetyl)-3,8-diaza-bicyclo[3.2.1]octane-8-carboxylic acid tert-butyl ester in DCM (4 mL) was added TFA (1 mL) and the solution stirred at RT for 1 h. The reaction mixture was concentrated in vacuo to give the title compound as a colourless oil (212 mg, 66%).