反応 #541221

反応方程式

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

2,3-dimethyl-5-hydroxyindole

→

4-(2,3-dimethylindol-5-yloxy)-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazoline

収率 40.0%

反応条件

後処理

1. 1
   その他(prepared
2. 2
   その他The crude product was purified by column chromatography
3. 3
   洗浄eluting with methanol/methylene chloride (1/9)

実験手順

Using an analogous procedure to that described in Example 34, 4-chloro-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazoline (110 mg, 0.34 mmol), (prepared as described for the starting material in Example 10), was reacted with 2,3-dimethyl-5-hydroxyindole (66 mg, 0.41 mmol), (Arch. Pharm. 1972, 305, 159). The crude product was purified by column chromatography eluting with methanol/methylene chloride (1/9) followed by 3M ammonia in methanol/methanol/methylene chloride (5/15/80) to give 4-(2,3-dimethylindol-5-yloxy)-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazoline (60 mg, 40%).

出典