| 摘要 |
NEW MATERIAL:The 7beta-arylmalonamide-3-( hetero cyclic )thiomethyl-1-dethia-1- oxa-3-cephem-4-carboxylic acid of formula I (Ar is phenyl, lower alkanoyloxyphenyl, carbamoyloxyphenyl, or thienyl; E is H or methoxy; Het is 1-methyl-5- tetrazolyl or 2-methyl-1,3,4-thiadiazol-5-yl; R is H or indanyl) or its salt. EXAMPLE:7alpha-Benzamido-3-( 1-methyltetrazol-5-yl )thiomethyl-1-dethia-1-oxa-3-cephem-4-carboxylic acid of formula II. USE:An antibacterial agent and its intermediate. PROCESS:The objective compound can be prepared by reacting the halomethyl compound of formula III with the thiol compound (salt) of formula Het-SH in an inert polar solvent such as amide, sulfoxide, etc. preferably DMF, etc., under cooling or at room temperature. |
