反应详情

温度

50 °C

6-Bromo-3-(quinolin-3-yl)-5-(1,2,3,6-tetrahydropyridin-4-yl)pyrazolo[1,5-a]pyrimidin-7-amine (0.035 mmol) was charged to a 20 mL scintillation vial. Then DMF (1 ml), N,N-diisopropylethylamine (0.14 mmol, 25 μL), and tert-butyl 2-bromoacetate (0.035 mmol, 5.2 μL) were added, respectively. The resulting reaction mixture was stirred at 50° C. 18 hours. After 18 hours, the reaction was concentrated in vacuo and treated with 1 mL TFA. This reaction mixture was stirred at room temperature for 2 hours. The reaction mixture was concentrated in vacuo and purified via reverse-phase preparatory HPLC to yield 2-(4-(7-amino-6-bromo-3-(quinolin-3-yl)pyrazolo[1,5-a]pyrimidin-5-yl)-5,6-dihydropyridin-1(2H)-yl)acetic acid as yellow solid. (m+H=479.17, retention time=2.09 min)

1. customThe resulting reaction mixture
2. custom18 hours
3. concentrationthe reaction was concentrated in vacuo
4. additiontreated with 1 mL TFA
5. stirringThis reaction mixture was stirred at room temperature for 2 hours
6. concentrationThe reaction mixture was concentrated in vacuo
7. custompurified via reverse-phase preparatory HPLC