Iodoacetamide → HCID 69291846, compound

Participants

Reaction Conditions

Reaction Steps

To a stirred solution of (RS)-(2-amino-4-cyano-benzyl)-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamide (470 mg) in DMF (8 ml) were added iodoacetamide (376 mg) and N-ethyldiisopropylamine (0.34 ml). After 50 hrs stirring at 110° C. under argon atmosphere. The mixture was diluted with EtOAc and water. The organic phase was separated and washed with water and brine, dried ovef MgSO4, filtered and concentrated. The crude product was purified by flash chromatography (CH2Cl2=>CH2Cl2/MeOH 4:1) to give (RS)-[2-(carbamoylmethyl-amino)-4-cyano-benzyl]-2-ethoxy-2-(2-fluoro-4-methoxy-phenyl)-acetamide (133 mg) as an off-white solid. MS 415.1([M+H]+)

Provenance & Evidence