反应详情

(E)-4-Hydroxypent-2-enoic acid (67 mg, 0.52 mmol) was dissolved in anhydrous DMF (2.5 ml), DCC (107.5, 0.52 mmol) and HOAt (106.7 mg, 0.79 mmol) were added and the mixture was stirred at room temperature for 15 minutes. 2-Methyl-4-piperazin-1-yl-quinoline (118.2 mg, 0.52 mmol) was added and stirring was continued for 90 minutes. The mixture was evaporated to dryness, taken up in a mixture of acetonitrile and methanol and filtered. The filtrate was evaporated to dryness again and purified by preparative HPLC (gradient of water containing 0.1% TFA and acetonitrile). 110 mg were obtained (0.33 mmol, 65%). MS (ES): m/z=326.1 [M+1]+.

1. stirringstirring
2. waitwas continued for 90 minutes
3. customThe mixture was evaporated to dryness
4. additiontaken up in a mixture of acetonitrile and methanol
5. filtrationfiltered
6. customThe filtrate was evaporated to dryness again
7. custompurified by preparative HPLC (gradient of water containing 0.1% TFA and acetonitrile)
8. custom110 mg were obtained (0.33 mmol, 65%)