反应详情

温度

60 °C

2-(Isopropylamino-thiazol-4-yl)-7-methoxy-quinolin-4-ol (220 mg, 0.7 mmol) (prepared as described in WO 00/59929) was dissolved in 7 ml of NMP (N-methyl pyrrolidinone), one spoon of Cs2CO3 was added, stirred at 60° C. for 1.5 h. Then compound 108 (150 mg, 0.24 mmol) was added. The reaction mixture was stirred at 80° C. overnight. Was diluted with chloroform and washed with sodium bicarbonate, brine. Water phases were back-extracted with chloroform. The combined organic layers were dried over sodium sulphate and evaporated. The crude product was purified by preparative HPLC (Gilson) (MeOH—H2O, 65%) to give 21 mg of product (yield 13%) as well as 12 mg of isomer.

1. stirringThe reaction mixture was stirred at 80° C. overnight
2. washwashed with sodium bicarbonate, brine
3. extractionWater phases were back-extracted with chloroform
4. dry with materialThe combined organic layers were dried over sodium sulphate
5. customevaporated
6. customThe crude product was purified by preparative HPLC (Gilson) (MeOH—H2O, 65%)