| 摘要 |
<p>NEW MATERIAL:2-Acetoxy-4-aryl-3-oxobutanoic acid derivative of formula I (R1 is H, hydroxyl or protected hydroxyl; R2 is a protecting group of carboxylic acid). EXAMPLE:Methyl 2-acetoxy-3-oxo-4-phenylbutanoate. USE:Intermediate for the synthesis of bestatin having a strong inhibitory action against aminopeptidase B, leucine aminopeptidase and bleomycin hydrolase. PROCESS:Compound of formula I is obtained by the acetoxylation of 4-aryl-3-oxobutanoic acid derivative of formula II, preferably using lead tetraacetate, mercury acetate, etc., in a solvent such as benzene or acetic acid at 0-100 deg.C. When lead tetraacetate is used, its amount is pref. about 1-1.2 moles per mole of the raw material.</p> |
