| abstract |
The invention provides processes for the preparation of compounds having the structure (QL ^) - L- (L ^ -B), where (1) Q is a quinolone unit, (II) B is a lactam unit, and (III) L, L ^ and 1 ? together constitutes a bonding unit, comprising the steps of: (1) coupling a compound of formula (III) with a lactam-containing compound to form an intermediate compound, and (2) cyclizing the intermediate by reaction with an organosilicon compound to to give a compound of formula (QL ^) - L- (L ^ -B). The process additionally further comprises a step of the coupling step, in which molded forms of the compound of formula (III) and the lactam compound are formed, and the deprotection step after the ring formation step, where the protecting groups are removed. Preferred antimicrobial compounds prepared by these methods are those wherein the β-lactam moiety is penem, carbapenem, cephem or carbacemefem. The compounds where L 1, L and L 3 form a carbamate unit, or a secondary or tertiary amine unit are also preferred. The invention also provides new intermediate compounds with 0 Q R? formula (M-L ^) - L- (L ^ -B) where (I) M has a structure of formula (IV), (II) B ¿. ,. ^. is a lactam moiety, and (III) L, L and L together form a binding moiety. |