| 摘要 |
PURPOSE:To prepare a beta-lactam derivative useful as an antibacterial agent with a versatile method, by reacting a novel sulfone compound with a thiol compound. CONSTITUTION:The beta-lactam compound of formula II can be prepared by reacting the sulfone compound of formula I [R1 is H or methyl; R2 is H, (protected) OH or (protected) CH2OH; R3 is H or together with R1 form a single bond; R4 is -CH2CH2- or -CH=CH-; R5 is ester residue; Y is protected NH2] with the thiol compound of formula R6-SH (R6 is H or univalent organic group) or its reactive derivative in an inert polar solvent preferably DMF, etc. at -30--50 deg.C. All the sulfone compounds of formula I are novel except the compound of formula III (Z is protected OH), and can be obtained e.g. by the S-oxidation of the compound of formula IV (m is 0 or 1). |
