反应详情

To a solution of 3-[(tert-butoxycarbonyl)amino]-2-hydroxypropanoic acid (1.61 g) in dichloromethane (8 ml) and tetrahydrofuran (8 ml) were added HOBT (1.59 g) and WSCD HCl (3.01 g), and the mixture was stirred at room temperature for 1 hour. The solution was cooled to 0° C., and 1-methyl-1H-pyrazole-4,5-diamine sulfate and N,N-diisopropylethylamine (4.1 ml) were added. The mixture was stirred at room temperature for 8 hours. The solvent was removed under reduced pressure to give crude tert-butyl {3-[(5-amino-1-methyl-1H-pyrazol-4-yl)amino]-2-hydroxy-3-oxopropyl}carbamate, which was used in the next reaction without further purification.

1. temperatureThe solution was cooled to 0° C.
2. stirringThe mixture was stirred at room temperature for 8 hours
3. customThe solvent was removed under reduced pressure