反応 #721861

反応方程式

hydrochloric acid

4-(5-benzyloxy-2-fluoro4-methylanilino)-7-hydroxy-6-methoxyquinazoline

2-bromoethanol

potassium carbonate

2-bromoethanol

potassium carbonate

→

4-(5-benzyloxy-2-fluoro-4-methylanilino)-7-(2-hydroxyethoxy)-6-methoxyquinazoline

収率 44.5%

溶媒

DMF

water

反応条件

後処理

1. 1
   温度the mixture was maintained at 50° C. for 2 hours
2. 2
   抽出extracted with ethyl acetate
3. 3
   乾燥The extracts were dried (MgSO4)
4. 4
   その他the solvent removed by evaporation
5. 5
   その他the residue triturated with ether and hexane

実験手順

A mixture of 4-(5-benzyloxy-2-fluoro4-methylanilino)-7-hydroxy-6-methoxyquinazoline (440 mg, 1 mmol), 2-bromoethanol (77 ml, 1 mmol) and potassium carbonate (150 mg, 1.1 mmol) in DMF (5 ml) was heated at 50° C. for 1 hour, further 2-bromoethanol (42 ml, 0.6 mmol) and potassium carbonate (150 mg, 1.1 mmol) was added and the mixture was maintained at 50° C. for 2 hours. The reaction mixture was diluted with water, neutralised with 2M hydrochloric acid and extracted with ethyl acetate. The extracts were dried (MgSO4), the solvent removed by evaporation and the residue triturated with ether and hexane to give 4-(5-benzyloxy-2-fluoro-4-methylanilino)-7-(2-hydroxyethoxy)-6-methoxyquinazoline (200 mg, 41%).

出典