| 摘要 |
NEW MATERIAL:Penem derivatives of formula I [R<1> is amino, hydroxyl, carbamoyl, group of R<2>-N=C(R<3>)-NH-(R<2> and R<3> are H, alkyl); A is alkylene] and their pharmacologically permissible salts or their biologically active esters. EXAMPLE:6-( 1'-Hydroxyethyl )-2-aminomethyl-2-penem-3-carboxylic acid or its sodium salt. USE:Antibiotic: they show antibiotic activities against a wide range of pathogenic bacteria including gram-positive and -negative bacteria. These compounds are modeled on thienamycin of strong antibiotic activity. PREPARATION:The phosphonium ylide of formula 5 (R<1>' is protected amino group; R<4> is hydroxyl-protecting group; R<5> is protecting group; R<6> is alkyl, acryl) is heated to give a compound of formula 6 and protecting groups are removed from the compound of formula 6 to produce the compound of formula I. |
