| 摘要 |
PROBLEM TO BE SOLVED: To obtain a highly safe carbapenem compound having a high antibacterial activity, exhibiting safe and excellent pharmacokinetics in vivo, also usable orally, by synthesizing a compound characteristic in terms of chemical structure. SOLUTION: This new compound is a carbapenem compound of formula I [R<1> is a (substituted) lower alkyl; R<2> is H or a lower alkyl; Y is a lone pair or (substituted) lower alkylene; R is a (hydrogenated) condensed oxazine, etc.], e.g. 6-hydroxy-6,7-dihydro-5H-imidazo[2,1-b][1,3]thiazine. The compound of formula I to be used as a medicine as an antibacterial agent is obtained by reaction of a compound of formula II (L is an eliminable group) or ester or salt thereof with a compound of the formula H-S-Y-R or salt thereof normally at -40 to 100 deg.C, pref. at -30 to 50 deg.C normally for 1min to 48h, pref. for about 15min to 48h in the presence of a base in an inert solvent under agitation. |
