反応 #40359

反応方程式

methyl ethyl amine

[4-(4-Amino-2,5-dimethyl-phenoxy)-pyrimidin-2-yl]-methyl-phenyl-amine

trimethoxymethane

p-toluene sulfonic acid

→

N′-{2,5-dimethyl-4-[2-(methyl-phenyl-amino)-pyrimidin-4-yloxy]-phenyl}-N-ethyl-N-methyl-formamidine

反応条件

後処理

1. 1
   workup.ADDITIONwere added
2. 2
   温度The reaction mixture was refluxed for 2 hrs
3. 3
   濃縮concentrated in vacuo
4. 4
   その他was evaporated
5. 5
   その他yielded 280 mg (89%) with a purity of 87%

実験手順

To a mixture of 252 mg (0.7 mmol) of [4-(4-Amino-2,5-dimethyl-phenoxy)-pyrimidin-2-yl]-methyl-phenyl-amine and 4 ml of trimethoxymethane, 20 mg of p-toluene sulfonic acid were added. The reaction mixture was refluxed for 2 hrs and concentrated in vacuo. The mixture was solved in 10 ml of dichloromethane and 62 mg (1.05 mmol) methyl ethyl amine was added. After stirring 18 hrs at ambient temperature the mixture was evaporated and yielded 280 mg (89%) with a purity of 87%; log P (pH 2.3)=1.61.

出典