反应详情

A solution of 80 mg (0.20 mmol) of rac-(1-{[(7-hydroxy-2,5-dimethylpyrazolo[1,5-a]pyridin-3-yl)carbonyl]amino}-2-methylpentan-2-yl)carbamic acid tert-butyl ester from Example 141A and 56 mg (0.27 mmol) of 3-(chloromethyl)-2,4-difluorobenzonitrile from Example 135A in 3 ml of DMF was admixed with 129 mg (0.396 mmol) of caesium carbonate. The resulting suspension was stirred at RT for 72 h and then diluted with dichloromethane (15 ml) and extracted with saturated aqueous sodium hydrogencarbonate solution (10 ml). The organic phase was concentrated under reduced pressure, which gave a crude product that contained the target compound in a multicomponent mixture (20% pure). This crude material was used in the next step without further purification.

1. extractionextracted with saturated aqueous sodium hydrogencarbonate solution (10 ml)
2. concentrationThe organic phase was concentrated under reduced pressure, which