| abstract |
NEW MATERIAL:Threo-(2RS)-3-amino-2-hydroxy-4-oxo-4-phenylbutyric acid and its ester of formula I (R1 is H or OH; R2 is protected amino; R3 is H or ester residue). EXAMPLE:Threo-(2RS)-3-acetylamino-2-hydroxy-4-oxo-4-phenylbutyric acid. USE:Raw material of (2S,3R)-3-amino-2-hydroxy-4-phenylbutyric acid and its derivative, which is a constituent amino acid of a carcinostatic agent, bestatin. PROCESS:The compound I is prepared by reacting 2-oxo-2-phenylethylamine derivative II with glyoxylic acid or its ester III in a solvent such as alcohol, in the presence of a base such as KOH. |