Hydrochloric Acid → 4-[(4E)-3-[2-(4-Carboxyphenyl)ethyl]-5-{5-fluoro-2-[3-(2-oxopyrrolidin-1-yl)propoxy]phenyl}-pent-4-en-1-yl]benzoic acid

Participants

Reaction Conditions

Reaction Steps

18 mg (0.75 mmol) of lithium hydroxide are added to a solution of 150 mg (0.25 mmol) of methyl 4-[(4E)-5-{5-fluoro-2-[3-(2-oxopyrrolidin-1-yl)propoxy]phenyl}-3-{2-[4-(methoxycarbonyl)-phenyl]ethyl}pent-4-en-1-yl]benzoate in 10 ml of THF and 10 ml of water, and the mixture is stirred at 50° C. for 12 h. The mixture is then adjusted to pH 2 using 1 M hydrochloric acid and concentrated. The residue obtained is purified directly by preparative HPLC. This gives 130 mg (content 96%, 0.22 mmol, 87% of theory) of the title compound.

Provenance & Evidence