Triethylamine → 4-[(1E)-3-tert-butoxy-3-oxoprop-1-enyl]-2-{[(5-methoxy-2-methyl-1H-indol-3-yl)acetyl]amino}benzoic acid

Participants

Reaction Conditions

Reaction Steps

To methyl 4-bromo-2-{[(5-methoxy-2-methyl-1H-indol-3-yl)acetyl]amino}benzoate (20 mg) was added palladium acetate (2 mg), tri-o-tolylphosphine (3 mg), t-butyl acrylate (33 μl), triethylamine (32 μl) and dimethylformamide (1 ml). After heating at 110° C. for 18 h, the solvent was removed in vacuo and the residue diluted with dichloromethane (10 ml) and washed with 5% citric acid (5 ml). Purification by SPE eluting with dichloromethane, chloroform, and chloroform: ether mixtures afforded the title compound (5 mg), MH+ 465; MH− 463; TR 4.47 min.

Provenance & Evidence