反応 #721863

反応方程式

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

hydrogen

→

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

収率 42.2%

溶媒

ethyl acetate

反応条件

後処理

1. 1
   その他(prepared
2. 2
   その他The catalyst was removed by filtration through diatomaceous earth and most of the solvent
3. 3
   その他removed by evaporation and hexane
4. 4
   workup.ADDITIONadded to the residue
5. 5
   ろ過The resulting precipitate was collected by filtration
6. 6
   その他dried

実験手順

A mixture of 4-(5-benzyloxy-2-fluoro-4-methylanilino)-7-(2-hydroxyethoxy)-6-methoxyquinazoline (150 mg, 0.33 mmol), (prepared as described for the starting material in Example 13), and 10% palladium-on-charcoal catalyst (20 mg) in ethyl acetate (8 ml) was stirred under 1 atmosphere of hydrogen at ambient temperature for 18 hours. The catalyst was removed by filtration through diatomaceous earth and most of the solvent removed by evaporation and hexane added to the residue. The resulting precipitate was collected by filtration and dried to give 4-(2-fluoro-5-hydroxy-4-methylanilino)-7-(2-hydroxyethoxy)-6-methoxyquinazoline (50 mg, 41%).

出典