| 摘要 |
<p>PURPOSE:To obtain the subject new compound useful as an antimicrobial agent, having stability to dehydropeptidase I and high recovery ratio in urine. CONSTITUTION:A compound of formula I {R<1> is H or methyl; R<2> is H, (substituted) lower alkyl, lower alkenyl, C(=NH)R<9> (R<9> is H or lower alkyl), etc.; R<10> are H or ester residue; A is group of formula II [(n) is 1-3; R<3> to R<5> are H, lower alkyl, etc.; R<6> and R<7> are H, halogen, (substituted) lower alkyl, OH, amino, etc.] or group of formula III [(m) is 0-2; (d) is 0 or 1; R<8> is H, (substituted) lower alkyl, etc.; R<9> is H, (substituted) lower alkyl, F, OH, etc.], etc.} such as (1R,5S,6S)-2-[(2S,4S)-2-(4-amidinopiperazin-1-ylcarbonyl)pyrrolidin-4- ylthio]-6-[(1R)-1-hydroxyethyl]-1-methyl-1-carbapen-2-em-3-carboxylic acid. The compound of formula I is synthesized from a compound of formula IV (R<14> is protecting group) through a compound such as a compound of formula V, etc.</p> |
