反応 #1898736

反応方程式

4-(6-chloro-5-methoxy-pyrimidin-4-yloxy)-piperidine-1-carboxylic acid isopropyl ester

potassium carbonate

4-bromo-2-fluorophenol

→

4-[6-(4-bromo-2-fluoro-phenoxy)-5-methoxy-pyrimidin-4-yloxy]-piperidine-1-carboxylic acid isopropyl ester

収率 35.0%

溶媒

DMA

反応条件

後処理

1. 1
   抽出The mixture was extracted with AcOEt and brine
2. 2
   乾燥Organic phase was dried over MgSO4
3. 3
   ろ過filtered
4. 4
   濃縮concentrated
5. 5
   その他The residue was purified by HPLC

実験手順

A mixture of 4-(6-chloro-5-methoxy-pyrimidin-4-yloxy)-piperidine-1-carboxylic acid isopropyl ester (2.19 g, 6.7 mmol), potassium carbonate (1.84 g, 13.3 mmol), and 4-bromo-2-fluorophenol (1.65 g, 8.65 mmol) in 32 ml DMA was heated at 160° C. for 5 hours. The mixture was extracted with AcOEt and brine. Organic phase was dried over MgSO4, filtered and concentrated. The residue was purified by HPLC to give 4-[6-(4-bromo-2-fluoro-phenoxy)-5-methoxy-pyrimidin-4-yloxy]-piperidine-1-carboxylic acid isopropyl ester as an oil (1.12 g, 35%). Exact mass calculated for C20H23BrFN3O5 483.08. found 484.4 (MH+).

出典