Yield: 98%

Reaction Conditions:

with hydrogenchloride in ethanol

Steps:

1 L-Melphalanyl-L-p-fluorophenylalanine ethyl ester hydrochloride (J1)
Example 1 L-Melphalanyl-L-p-fluorophenylalanine ethyl ester hydrochloride (J1) L-p-Fluorophenylalanine (217 mg, 1.18 mmol) was dissolved in EtOH (5 ml) previously bubbled with HCl. The reaction was brought to 100° C. and was allowed to reflux for 18 hours. The solvent was evaporated off and the product was dried under high vacuum, affording L-p-fluorophenylalanine ethyl ester hydrochloride as dry white crystals (98%). ¹H NMR: (CD₃OD) δ 7.30-7.26 (m, 2H, Ph-H), 7.13-7.06 (m, 2H, Ph-H), 4.29-4.22 (m, 2H, CH₂-Ph), 3.31-3.10 (m, 3H, CH₂CH₃, α-H), 1.24 (t, 3H, CH₂CH₃).

References:

Lewensohn, Rolf;Gullbo, Joakim;Larsson, Rolf;Ehrsson, Hans;Luthman, Kristina US2004/97421, 2004, A1

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