| 摘要 |
<p>PROBLEM TO BE SOLVED: To obtain a new penem derivative useful as an antimicrobial agent, especially as an antibiotic substance effective against methicillin resistant Staphylococcus aureus(MRSA). SOLUTION: This new penem derivative is represented by formula I (Z is OH or F; R1 ', is an alkyl, an alkenyl, an aralkyl, an aryl, a heterocyclic ring, an acyl or H; R2 is H or a carboxyl-protecting group), e.g. p-nitrobenzyl 2-[(3R,4 S)-3-((R)-1-tert-butyldimethylsilyloxyethyl)-4-phenylthio-2-azetidinon -1-yl]acetate. The compound represented by formula I is obtained by reacting a compound represented by formula II (Z' is a protected hydroxyl group represented by OR3 or F; R4 is a protecting group of carboxyl) with a compound represented by the formula X-R5 (X is a halogen, an alkanesulfonyloxy, etc.; R5 is an alkyl, an alkenyl, an aralkyl, etc.), providing a compound represented by formula III and then deprotecting the resultant compound represented by formula III. The daily dose thereof is 50mg to 5g/adult in the case of peroral administration.</p> |
