| 摘要 |
NEW MATERIAL:A compound of formula I [R1 is H, trialkylsilyl; R2 is H, trialkylsilyl, carboxyl or esterified carboxyl], its salt or ester. EXAMPLE:2beta-( 4-Ethoxycarbonyl-1, 2, 3-triazol-1-yl)methyl-2alpha-methylpenam-3alpha-carboxylic acid-1,1-dioxide p-nitrobenzyl ester. USE:beta-Lactamase inhibitor. PREPARATION:For example, the reaction of 1mol of a penicillanic acid derivative of formula II with 1-10mol of an acetylene derivative of formula III gives a compound of formula IV. Then, the compound is deesterified by, e.g., hydrolysis to give a compound of formula V where R2 in formula I is R4 (R4 is R2 other than H). The compound of formula II as the starting substance is novel and obtained by reaction of a compound of formula VI (X is chlorine, bromine; R is protecting group for penicillin carboxyl) with a metal azide and followed by oxidation. |
