| 摘要 |
The present invention provides processes for making compounds of the structure(Q-L1)-L-(L2-B)wherein (I) Q is a quinolone moiety; (II) B is a lactam moiety; and (III) L, L1, and L2 together comprise a linking moiety; 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 give a compound of the formula (Q-L1)-L-(L2-B). Preferably, the process 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, wherein the protecting groups are removed. Preferred antimicrobial compounds made by these processes are those where the beta-lactam moiety is a penem, a carbapenem, a cephem, or a carbacephem. Also preferred are those compounds where L1, L, and L2 form a carbamate moiety, or a secondary or tertiary amine moiety. The present invention also provides novel intermediate compounds of the formula(M-L1)-L-(L2-B),where (I) M has a structure according to formula (IV) <IMAGE> (IV) (II) B is a lactam moiety; and (III) L, L1, and L2 together comprise a linking moiety.
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