Morpholine → 5-Morpholino-2-nitroaniline

Participants

Reaction Conditions

Reaction Steps

To a solution of morpholine (0.88 mL) and 5-chloro-2-nitroaniline (1.76 g) in DMF (50 mL) was added TEA (2.78 mL). The mixture was stirred at 120° C. overnight, cooled down and the solvent was removed in vacuo. The residue was purified by CC (Biotage, SNAP 50 g cartridge, solvent A: Hept; solvent B: EA; gradient in % B: 10 for 3CV, 10 to 30 over 6CV, 30 for 2CV, 30 to 50 over 4CV, 50 for 6CV) to afford 380 mg of yellow powder. LC-MS (B): tR=0.69 min; [M+H]+: 224.15.

Provenance & Evidence