反应详情

88 mg (0.17 mmol) of tert-butyl (3R)-3-[({7-[(2,6-difluorobenzyl)oxy]-2,5-dimethylpyrazolo[1,5-a]pyridin-3-yl}carbonyl)amino]-5-methylhexanoate from Example 37 were suspended in 2 ml of diethyl ether and admixed with 2.56 ml of 2 N hydrogen chloride solution, and the mixture was stirred at RT overnight. Subsequently, 2 ml of 2 N hydrogen chloride solution in diethyl ether were added and the mixture was stirred at RT for 4 h. The reaction mixture was concentrated, admixed with water and TFA and purified by means of preparative HPLC (RP18 column, eluent:acetonitrile/water gradient with addition of 0.1% TFA). The product fractions were combined, concentrated and lyophilized. 57 mg of the target compound were obtained (73% of theory).

1. stirringthe mixture was stirred at RT for 4 h
2. concentrationThe reaction mixture was concentrated
3. custompurified by means of preparative HPLC (RP18 column, eluent:acetonitrile/water gradient with addition of 0.1% TFA)
4. concentrationconcentrated