1-piperidin-4-ylpiperidin-2-one;hydrochloride

反応条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: To a solution of 2-(2-fluorophenyl)-2-(4-chlorophenylaminocarbonylamino)-acetic acid (45 mg, 0.14 mmol), 4-(2-piperidinon-1-yl)piperidine hydrochloride (40 mg, 0.18 mmol) and triethylamine (0.085 mL, 0.61 mmol) in DMF (1.0 mL, containing 0.050 mL of H2O to solubilize the piperidine hydrochloride), BOP (100 mg, 0.23 mmol) was added. After being stirred at room temperature for 30 min, the mixture was purified by HPLC to give the titled compound (20 mg). MS 487.3 and 489.3 (M+H, Cl pattern). was added the mixture was purified by HPLC

反応条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: To a solution of 2-(2-fluorophenyl)-2-(4-chlorophenylaminocarbonylamino)-acetic acid (45 mg, 0.14 mmol), 4-(2-piperidinon-1-yl)piperidine hydrochloride (40 mg, 0.18 mmol) and triethylamine (0.085 mL, 0.61 mmol) in DMF (1.0 mL, containing 0.050 mL of H2O to solubilize the piperidine hydrochloride), BOP (100 mg, 0.23 mmol) was added. After being stirred at room temperature for 30 min, the mixture was purified by HPLC to give the titled compound (20 mg). MS 487.3 and 489.3 (M+H, Cl pattern). was added the mixture was purified by HPLC

反応条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: To a solution of(D) N-BOC phenylglycine (32 mg, 0.13 mmol), 4-(2-piperidinon-1-yl)piperidine hydrochloride (22 mg, 0.10 mmol) and triethylamine (0.070 mL, 0.50 mmol) in DMF (1.0 mL), BOP (66 mg, 0.15 mmol) was added. The mixture was stirred at room temperature for 20 min. Water and EtOAc were added. The EtOAc phase was separated, washed with 5% NaHCO3, dried over Na2SO4, and concentrated in vacuo to give the amide (51 mg). MS 416.5 (M+H). The EtOAc phase was separated washed with 5% NaHCO3 dried over Na2SO4 concentrated in vacuo

反応条件: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

実験手順: To a solution of(D) N-BOC phenylglycine (32 mg, 0.13 mmol), 4-(2-piperidinon-1-yl)piperidine hydrochloride (22 mg, 0.10 mmol) and triethylamine (0.070 mL, 0.50 mmol) in DMF (1.0 mL), BOP (66 mg, 0.15 mmol) was added. The mixture was stirred at room temperature for 20 min. Water and EtOAc were added. The EtOAc phase was separated, washed with 5% NaHCO3, dried over Na2SO4, and concentrated in vacuo to give the amide (51 mg). MS 416.5 (M+H). The EtOAc phase was separated washed with 5% NaHCO3 dried over Na2SO4 concentrated in vacuo