Acetic acid 2-[1-{2-[2-acetylamino-3-(hydroxyphenyl)propionyl-amino]-3-(4-fluorophenyl)propionyl}-4-(1-methylcarbamoyl-2-naphthalen-2-ylethyl)-piperazin-2-yl]ethyl ester → 2-[4-[2-[2-Acetylamino-3-(4-hydroxyphenyl)propionylamino]-3-(4-fluorophenyl)propionyl]-3-(2-hydroxyethyl)piperazin-1-yl]-n-methyl-3-naphthalene-2-yl-propionamide

Participants

Reaction Steps

To a solution acetic acid 2-[1-{2-[2-acetylamino-3-(hydroxyphenyl)-propionylamino]-3-(4-fluorophenyl)propionyl}-4-(1-methylcarbamoyl-2-naphthalen-2-ylethyl)-piperazin-2-yl]ethyl ester, 65, (7.5 g, 10 mmol) in methanol (50 mL) is added freshly prepared NaOCH3 (0.55 g, 10.1 mmol) and the solution stirred overnight. The solution is concentrated in vacuo, the resulting residue partitioned between dichloromethane and water, the organic layer is dried and concentrated in vacuo to afford the desired product.

Provenance & Evidence