反应详情

1-{3-[4-(3-Methyl-2-oxo-2,3-dihydro-benzoimidazol-1-yl)-piperidin-1-yl]-propyl}-3-(4-trifluoromethyl-phenyl)-1,4,6,7-tetrahydro-pyrazolo[4,3-c]pyridine-5-carboxylic acid tert-butyl ester (1.19 g, 1.86 mmol) was dissolved in trifluoroacetic acid (5 mL) and CH2Cl2 (5 mL) and allowed to stir at room temperature for 2 h. The reaction mixture was concentrated, diluted with CH2Cl2, and washed with saturated NaHCO3. The organic layer was dried over Na2SO4 and concentrated to afford 1-methyl-3-(1-{3-[3-(4-trifluoromethyl-phenyl)-4,5,6,7-tetrahydro-pyrazolo[4,3-c]pyridin-1-yl]-propyl}-piperidin-4-yl)-1,3-dihydro-benzoimidazol-2-one (0.955 g, 96%) as a white foam. TLC (silica, 10% MeOH/CH2Cl2): Rf=0.19. MS (electrospray) calculated for C29H33F3N6O, 539.3 ([M+H]+). m/z found, 539.3.

1. concentrationThe reaction mixture was concentrated
2. additiondiluted with CH2Cl2
3. washwashed with saturated NaHCO3
4. dry with materialThe organic layer was dried over Na2SO4
5. concentrationconcentrated