| 摘要 |
NEW MATERIAL:A compound of formulaI[R<1> is H, lower alkyl bearing hydroxyls as substituents; R<2> is cyclic amino of 3-7 membered ring including or not including O, S in the ring wherein the N may have a group of formula II (R<4>, R<5> are H, lower alkylene); R<3> is H, ester residue; A is single bond or lower alkylene]and its salt. EXAMPLE:6-(1-Hydroxyethyl)-2-(aziridin-2-yl)-2-penem-3-carboxylic acid. USE:Antibacterial: it shows high activity against gram-positive and gram-negative bacteria. PREPARATION:A compound of formula III (R<6> is H, lower alkyl bearing protected hydroxyls as substituents; R<7> is cyclic amine corresponding to R<2> with the N protected; R<8> is a group protecting a carboxyl; R<9> is alkyl) is heated to give a compound of formula IV, which is subjected to deprotection of R<8> and of the protecting groups included in R<6> and R<7> to give the compound of formulaI. |
