Acetic Acid → Ethyl 3-amino-3-(3-{[(3-{[(propylamino)carbonyl]amino}phenyl)sulfonyl]amino}phenyl)propanoate

Participants

Reaction Steps

2.57 ml of acetic acid, 5.32 ml of tributyltin hydride and 177 mg of bis(triphenyl phosphine) palladium(II) chloride were added to a solution of 9.58 g of ethyl 3-{[(allyloxy)-carbonyl]-amino}-3-{{3-{[(3-{[(propylamino)-carbonyl]-amino}-phenyl)-sulphonyl]-amino}-phenyl}}-propanoate from Example II.2.g in 245 ml of dichloromethane, and the resultant mixture was stirred at room temperature for 22 h. An aqueous solution of sodium bicarbonate was added, and the mixture was extracted with dichloromethane. After drying the organic phase over magnesium sulphate, the solvent was removed, and the crude product was purified by chromatography on silica gel (dichloromethane/methanol=10:1) to give 2.30 g of the desired compound.

Provenance & Evidence