| 摘要 |
NEW MATERIAL:The compound of formula I [R1 and R2 are H, lower alkyl, phenyl (substituted with halogen, lower alkyl, etc.), lower acyl, cyano, formyl, -S(O)nR3 (R3 is lower alkyl; n is 0-2), -COOR4 (R4 is nitro-substituted benzyl, alkali metal, 7-18C alkyl, etc.), etc.; R1 and R2 are not H at the same time], its salt or its ester. EXAMPLE:2beta-( 4, 5-Dimethyl-1, 2, 3,-triazol-1-yl )methyl-2alpha-methylpenam-3alpha-carboxylic acid 1,1-dioxide sodium. USE:A beta-lactamase-inhibiting agent. PREPARATION:The objective compound can be produced by reacting the compound of formula II (R5 is protecting group of the penicillin carboxyl group) with preferably 1-10mol-equivalent of the acetylene derivative of formula III (R6 and R7 are same as R1 and R2), and if necessary, subjecting the reaction product to saponifying reaction, ester-exchange reaction, or salt-forming reaction. |
