反応 #325272

反応方程式

hydrogen chloride

4-chloro-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazoline

4-bromo-2-fluoroaniline

→

4-(4-bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazoline hydrochloride

収率 95.8%

溶媒

isopropanol

isopropanol

反応条件

後処理

1. 1
   温度was heated
2. 2
   温度at reflux for 1.5 hours
3. 3
   温度After cooling
4. 4
   ろ過the precipitate was collected by filtration
5. 5
   洗浄washed with isopropanol
6. 6
   その他dried under vacuum

実験手順

A suspension of 4-chloro-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazoline (200 mg, 0.62 mmol) and 4-bromo-2-fluoroaniline (142 mg, 0.74 mmol) in isopropanol (3 ml) containing 6N hydrogen chloride in isopropanol (110 μl, 0.68 ml) was heated at reflux for 1.5 hours. After cooling, the precipitate was collected by filtration, washed with isopropanol followed by ether and dried under vacuum to give 4-(4-bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazoline hydrochloride (304 mg, 90%).

出典