| 摘要 |
<p>PURPOSE:To provide a new carbapenem compound having powerful antibacterial activity on sensitive, resistant gram-positive and gram-negative bacteria and excellent stability to beta-lactamase and DHP-I, thus useful as an antibacterial agent. CONSTITUTION:The objective compound of formula I [R<1> is H or CH3; R<2> is H or negative charge; X is N(R<3>)R<4> or N<+> (R<5>) (R<6>) R<7>; R<3>-R<7> are each lower alkyl, besides, R<4> is H; n is 2, 3, or 4], or a pharmaceutically allowable salt or ester thereof, e.g. (1R, 5S, 6S)-6-[(R)-1-hydroxyethyl]-1-methyl-2-[(2R, 4S)-2-[2(methylmino)ethyl]pyrrolidine-4-ylthio]-1-carbapen-2-em-3-carb oxylic acid of formula II. The compound of the formula I can be obtained by reaction of a compound of formula III (R<8> and R<20> are each H or protecting group) with a compound of formula IV [R<9> is H or protecting group; X<1> is N(R<3>)R<40> or N<+>(R<5>) (R<6>)R<7>; R<40> is R<4> or protecting group] to produce a compound of formula V followed by, if needed, removing the protecting group from this compound.</p> |
