| 摘要 |
PURPOSE:To obtain the subject compound which is an important intermediate for the synthesis of carbapenems, in high yield and in a short step, by condensing a peracid to an azetidinon-2-one having carboxyl group or its derivative at 4-site and simultaneously carrying out the decarbonation reaction. CONSTITUTION:The objective 4-acyloxyazetidinon-2-one of formula III is produced by reacting a compound of formula I (R<1> is H or protecting group of amide nitrogen; R<2> is H, hydroxymethyl, etc.; R<3> is halogen, OH, acyloxy, etc.) (in a form dissolved in a solvent when R3 1a R) with a peracid of formula II (R<4> is methyl, CFS or phenyl) in the presence of a condensation agent. When R3 is not OR, the compound of formula I is dissolved in a solvent and made to react with a peracid in the presence of a base to obtain a compound of formula III (e.g., the compound of formula IV). The process has excellent industrial merits. |
