| 摘要 |
NEW MATERIAL:The compound of formula I [Cbz is benzyloxycarbonyl; R1 and R2 is H, substituted carboxyl or (substituted) alkyl or aryl]. EXAMPLE:2-Cbz amino-2-butenoic acid t-butyl ester. USE:Useful for the synthesis of a physiologically active substance containing abnormal amino acid residue using an alpha,beta-dehydroamino acid as a precursor. The physiologically active substances has antibacterial and antitumor activities. PREPARATION:The compound of formula I can be produced by dissolving a Cbz- alpha,beta-dehydroamino acid of formula II in a solvent such as dichloromethane, cooling the solution to <=0 deg.C, preferably to -20 deg.C, blasting isobutene gas into the solution to attain a supersaturated state and reacting the components in the presence of sulfuric acid in closed or pressurized system for several days.
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