Triethylamine → methyl 2-acetamido-3-[2-[(2R)-3-ethoxycarbonyl-2-(4-cyanobenzoylamino)propoxy]-4-cyanophenyl]acrylate

Participants

Reaction Conditions

Reaction Steps

1.28 g (2.27 mmol) of benzyl (3R)-4-(5-cyano-2-iodophenoxy)-3-(4-cyanobenzoylamino)butanoate, 975 mg (6.81 mmol) of methyl 2-acetamidoacrylate, 415 mg (1.36 mmol) of tris(2-methylphenyl)phosphine, 0.95 ml (6.81 mmol) of triethylamine and 0.5 ml of dimethylformamide were dissolved in 8.0 ml of acetonitrile. 56 mg (0.23 mmol) of palladium acetate was added to the solution at room temperature, and they were stirred at 90° C. for 12 hours. The solvent was distilled off, and the residue was purified by the silica gel column chromatography (volume ratio of chloroform:methanol=30:1) to obtain the title compound.

Provenance & Evidence