摘要 |
NEW MATERIAL:A compound of formula I [R<1> is H, alkyl, alkoxyl, etc.; R<2> is H or group of formula II (R<5> and R<6> are alkyl, aralkyl, aryl, etc.); R<3> is H or a protecting group of the caroboxl group] and a pharmacologically acceptable salt thereof. EXAMPLE:2-Thioxopenam-3-carboxylic acid. USE:An antimicrobial agent and a synthetic intermediate therefor effective against a wide range of pathogenic germs including Gram-positive Gram-negative bacteria. PROCESS:A compound of formula III (R<7> is H, alkyl, etc.; R<8> is lower alkyl; R<9> is a protecting group of the carboxyl group) is treated with a base and then reacted with CS2 and further reacted with a compound of the formula X-CO-X (X ishalopound of formula V (Y is halogen). The resultant compound is then cyclized with a base, and if necessary the protecting group is removed to afford the compound of formula I (R<2> is H). |