| abstract |
The present invention provides processes for producing compounds of the structure (Q-Lü) -L- (L²-B), wherein (I) Q is a quinolone entity; (II) B is a lactam entity; and (III) L, Lü, and L² together comprise a linking entity; They comprise the steps of: (1) coupling a compound of formula (III) with a lactam-containing compound to form an intermediate compound; and (2) cyclization of the intermediate by reaction with an organic silicon compound to give a compound of the formula (Q-Lü) -L- (L²-B); preferably, the method additionally comprises a step prior to the coupling step wherein protected forms of the compound of formula (III) and the lactam compound are formed; and deprotection steps after the cyclization step, where the protecting groups are removed; Preferred antimicrobial compounds produced by these procedures are those where the beta-lactam entity is a penem, a carbapenem, a cepheme, or a carbazepheme; Compounds in which Lü, L and L² form a carbamate entity, or a secondary or tertiary amine entity are also preferred; The present invention also provides novel intermediate compounds of the formula (M-Lü) -L- (L²-B), where (I) M has a structure according to formula (IV), (II) B is an entity lactam, and (III) L, Lü, and L² together comprise a binding entity. |