Formic Acid → 4-[Bis(2-chloroethyl)amino]-N-formyl-L-phenylalanine

Participants

Reaction Steps

A solution of 4-[bis(2-chloroethyl)amino]-(L)-phenylalanine (150 mg) in formic acid (1.82 ml) and acetic anhydride (0.64 ml) is stirred at room temperature for 3 hours. The reaction mixture is concentrated to reduced volume under reduced pressure and partitioned between water (3 ml) and ethyl acetate (2×50 ml). The organic phase is dried over sodium sulphate and the solvent is evaporated under vacuum, to give N-formyl-4-[bis(2-chloroethyl)amino]-(L)-phenylalanine (160 mg) as a yellow foam, [α]D =+67° (C=2, ethanol).

Provenance & Evidence