反应详情

124 mg (0.37 mmol) of 7-[(2,6-difluorobenzyl)oxy]-2,5-dimethylpyrazolo[1,5-a]pyridine-3-carboxylic acid from Example 4A were initially charged together with 184 mg (0.49 mmol) of HATU and 0.52 ml (3.00 mmol) of N,N-diisopropylethylamine in 1.24 ml of DMF, and the mixture was stirred at room temperature for 10 min. Subsequently, 175 mg (0.49 mmol) of tert-butyl [(1S)-1-{5-[(1S)-1-amino-2-hydroxyethyl]-1,3,4-oxadiazol-2-yl}-2-methylpropyl]carbamate acetate from Example 173A were added to the reaction solution and the mixture was stirred at RT for 1 h. Then the mixture was diluted with acetonitrile and water, admixed with TFA and purified by means of preparative HPLC (RP18 column, eluent:acetonitrile/water gradient with addition of 0.1% TFA). 211 mg of the target compound were obtained (73% of theory, 94% purity).

1. stirringthe mixture was stirred at RT for 1 h
2. custompurified by means of preparative HPLC (RP18 column, eluent:acetonitrile/water gradient with addition of 0.1% TFA)