| 摘要 |
NEW MATERIAL:An azetidinone derivative shown by formula I(R<1> is H or trialkylsilyl; R<2> is H or amino group-protecting group]. EXAMPLE:( 3SR,4SR,1'RS )-N-Dianisylmethyl-3-(1'-fluoroethyl)-4-tri-methylethynyl- 2-azetidinone. USE:An intermediate for producing fluorocarbapenem type beta-lactam antibiotic. The fluorocarbapenem antibiotic is much stable to enzymes in the kidney and shown improved antibacterial activity against Gram-positive and Gram-negative bacteria. PREPARATION:A diketene shown by formula II is reacted with an acetylene- imine shown by formula III in the presence of an imidazole to give a 3- acetylazetidinone derivative shown by formula IV, which is then stereoselectively reduced to give a hydroxy-azetidinone derivative shown by formula V, which is treated with a fluorinating agent to give a compound shown by formula I. |
