反应详情

N-methyl morpholine (1 eq) and chloroacetylchloride (1 eq) were added to a stirred solution of methyl 2-[3-(acetylamino)-2-aminophenyl]-3-cyclohexyl-1H-indole-6-carboxylate in CH2Cl2 (0.03 M) under N2. After stirring at RT for 1 h, further N-methyl morpholine (1 eq) and chloroacetylchloride (1 eq) were introduced. The reaction was stirred for another hour before diluting with CH2Cl2 and washing with 1N HCl (aq), water and brine. The organics were then dried over anhydrous sodium sulfate, filtered and concentrated in vacuo to afford the title compound as a brown solid that was taken on in the subsequent step without further purification (91%). MS (ES+) m/z 482 (M+H)+, 484 (M+H)+.

1. stirringThe reaction was stirred for another hour
2. washwashing with 1N HCl (aq), water and brine
3. dry with materialThe organics were then dried over anhydrous sodium sulfate
4. filtrationfiltered
5. concentrationconcentrated in vacuo