反応 #44273

反応方程式

6-[6-(1H-pyrazol-4-yl)-[1,2,3]triazolo[4,5-b]pyrazin-1-ylmethyl]-quinoline

Cs2CO3

2,2-dimethyl-oxirane

→

2-methyl-1-[4-(3-quinolin-6-ylmethyl-3H-[1,2,3]triazolo[4,5-b]pyrazin-5-yl)-pyrazol-1-yl]-propan-2-ol

収率 22.0%

溶媒

DMF

反応条件

後処理

1. 1
   その他The reaction was then purified with a reverse-phased preparative HPLC
2. 2
   洗浄eluting with acetonitrile-water having 0.1% acetic acid

実験手順

To a suspension of 6-[6-(1H-pyrazol-4-yl)-[1,2,3]triazolo[4,5-b]pyrazin-1-ylmethyl]-quinoline (50 mg, 0.15 mmol) and Cs2CO3 (50 mg, 0.15 mmol) in DMF (2 mL) was added 2,2-dimethyl-oxirane. The reaction was stirred at 80° C. for 16 hours. The reaction was then purified with a reverse-phased preparative HPLC eluting with acetonitrile-water having 0.1% acetic acid to yield 2-methyl-1-[4-(3-quinolin-6-ylmethyl-3H-[1,2,3]triazolo[4,5-b]pyrazin-5-yl)-pyrazol-1-yl]-propan-2-ol (13 mg, 22% yield).

出典