PURPOSE: To prepare the titled compound useful as an intermediate of an amino acid, etc., economically in an industrial scale, using single reactor without separating intermediate products, by treating an aspartic acid derivative with a halogenating agent and a base, and if necessary, further with an acid.
CONSTITUTION: An α-aminoacrylic acid derivative of formula I (R1 is H or ester residue; R2 is amino-protecting group) is prepared by treating an aspartic acid derivative of formula II with a halogenating agent (e.g. alkali hypochlorite, chlorine, etc.) and a base (e.g. NaOH, sodium carbonate, etc.) in an inert solvent such as water, ethanol, etc., and when the liquid is neutral or alkaline after the reaction, treating the liquid with an acid. When an alkali hypochlorite is used as the halogenating agent and the base, the compound of formula I can be obtained in one step and in high yield.
USE: An intermediate of α-mercapto-α-amino acid having antiviral activity.
MATSUMOTO KAZUO
MORIYA TAMON
