| 摘要 |
NEW MATERIAL:A beta-lactam compound shown by the formula I (R is H or lower alkyl). EXAMPLE:(5R, 6S)-2-[4 -( Formylimidoyl ) piperidinylthio]-6 -[(R)- 1-hydroxyethyl] penem-3-carboxylic acid. USE:An antibacterial agent. Showing improved activity against Gram-positive and Gram-negative bacteria. A dose is 200-300mg per adult daily. PROCESS:A penem-3-carboxylic acid compound shown by the formula II is reacted with a compound shown by the formula III (R1 is lower alkyl; Y is O or S) or a salt of its acid under an alkali condition at 0 deg.C- room temperature to give a compound shown by the formula I . The reaction under the alkali condition is carried out at 8-12pH, preferably at about 9-10 using an alkalizing agent such as sodium hydroxide, potassium hydroxide, etc. in an organic solvent. |
