| 摘要 |
NEW MATERIAL:A compound of formulaI[R<1> is hydrocarbon or heterocyclic group; R<2> is H or protecting group of OH; (n) is 0, 1 or 2; provided that (n) is 2 when R<1> is acetamidoethyl or acetamidoethenyl and R<2> is H or sulfonic acid] or a salt thereof. EXAMPLE:5, 6-cis-3-( 2-Aminoethylthio )-6-( 1-hydroxy-2-methylethyl )-7-oxo-1-azabicyclo[3.2.0]hept-1-ene-2-carboxylic acid. USE:An antimicrobial agent, exhibiting improved activity particularly against Gram-positive and Gram-negative bacteria, and useful as beta-lactamase inhibitors. PROCESS:A compound of formula II (R<3> is H or protecting group of the carboxyl group; X is eliminative group) or a salt thereof is reacted with a compound of the formula R<1> S(O)nH in a solvent, e.g. dichloromethane or tetrahydrofuran, at -50-+40 deg.C to give the compound of formlaI. |
