| 摘要 |
NEW MATERIAL:A compound of formula I (R<1> is aralkyl; R<3> is H or carboxyl- protecting group). EXAMPLE:(1R,5S,6S)-2-oxo-6-[(1R)-1-hydroxyethyl]-1-benzyloxycarbapenam -3-car boxylic acid p-nitrobenzyl ester. USE:An intermediate for antibacterial agent and beta-lactamase inhibiting agent. PREPARATION:An azetidin-2-one derivative of formula II (R<4> is OH-protecting group; R<5> is H, lower alkyl, aryl or aralkyl) is made to react with a magnesium malonate compound of formula (R<3>OOCH2CO2)Mg (R<3> is carboxyl-protecting group) in the presence of imidazole to obtain a compound of formula III. The protecting group of the group R<4> is eliminated to obtain a compound of formula IV, which is treated with an azide compound in the presence of a base. The resultant diazo compound of formula V is cyclized in the presence of a metal acetate catalyst. |
