| 摘要 |
NEW MATERIAL:The compound of formulaI[R<1> is H, alkyl, alkoxy, or R<4>A- (R<4> is OH, alkoxy, acyloxy, alkylsulfonyloxy, amino, etc.; A is CF3 or alkylene which may be substituted with phenyl); R<2> is cycloaliphatic amine residue; R<3> is H or carboxyl-protecting groupand its pharmacologically allowable salt. EXAMPLE:(5R,6S,8R)-6-(1-Hydroxyethyl)-2-(N-p-nitrobenzyloxycarbonyl-py rrolidin- 3-ylthio)-2-carbapenem-3-carboxylic acid p-nitrobenzyl ester. USE:Remedy for infectious diseases. Effective to Gram-position and Gram-negative bacteria. PROCESS:The compound of formula 2 is made to reaet with an alkanesulfonic acid anhydride in the presence of a base to obtain the compound of formula 3, which is made to react with a marcaptan in the presence of a base to obtain the compound of formula 5 and then the compound of formula 1. |
