反応 #1531309

反応方程式

4-(4-fluoro-phenyl)-6-(2-(R)-methyl-piperazin-1-yl)-2-(2-(R)-methyl-pyrrolidin-1-yl)-pyrimidine

2,5-dibromo-3-methyl-pyridine

DIEA

→

title compound

4-[4-(5-bromo-3-methyl-pyridin-2-yl)-2-(R)-methyl-piperazin-1-yl]-6-(4-fluoro-phenyl)-2-(2-(R)-methyl-pyrrolidin-1-yl)-pyrimidine

溶媒

DMA

water

反応条件

後処理

1. 1
   温度Heat
2. 2
   抽出extract with EtOAc
3. 3
   洗浄wash with brine
4. 4
   乾燥Dry the organic layer (Na2SO4)
5. 5
   濃縮concentrate under reduced pressure
6. 6
   その他Purify the residue by flash column chromatography
7. 7
   洗浄eluting with EtOAc-Hexanes (1:10)

実験手順

Heat a mixture of 4-(4-fluoro-phenyl)-6-(2-(R)-methyl-piperazin-1-yl)-2-(2-(R)-methyl-pyrrolidin-1-yl)-pyrimidine (400 mg, 1.13 mmol), 2,5-dibromo-3-methyl-pyridine (367 mg, 1.46 mmol), and DIEA (218 mg, 1.69 mmol) in DMA at 135° C. for 96 h. Dilute with water, extract with EtOAc, and wash with brine. Dry the organic layer (Na2SO4) and concentrate under reduced pressure. Purify the residue by flash column chromatography eluting with EtOAc-Hexanes (1:10) to afford the title compound as a white solid.

出典