abstract |
The present invention relates to a process for the preparation of 4- (substituted mercapto) -2-oxo-1-azetidine sulfonic acid salts of formula (I). Compounds of formula I wherein R is hydrogen or methoxy; R [acyl; R2 and R3 are independently hydrogen or alkyl, or together form a cycloalkyl with the carbon to which they are attached; R 4 is hydrogen, alkyl, aryl, pyridyl, furyl, thienyl, a or b or cyano; R5 is hydrogen, alkyl, aryl, aralkyl, hydroxyl, -O-M +, alkoxy, aryloxy or aralkoxy; R 'and R7 are independently hydrogen, alkyl, aryl or aralkyl; M + hydrogen or a cation is prepared by acylating compounds of formula VI wherein M + is hydrogen with reagents suitable for introduction of R 1 acyl. The compounds of the invention are active against Gram-positive and Gram-negative bacteria and can be used in human and veterinary medicine. 10 15 20 186490 Rr-NH NH. 3-CH-R-CH1-CH-N-S0- CH-CH-N-VI-1- |