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Title:
【発明の名称】キノロニルラクタム抗微生物剤の製造方法及び新規中間化合物
Document Type and Number:
Japanese Patent JPH10503521
Kind Code:
A
Abstract:
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) (IV) (II) B is a lactam moiety; and (III) L, L1, and L2 together comprise a linking moiety.

Inventors:
Randal, Jared Lynn
Godlewski, Jane Ellen
Application Number:
JP50667496A
Publication Date:
March 31, 1998
Filing Date:
August 01, 1995
Export Citation:
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Assignee:
THE PROCTER AND GAMBLE COMPANY
International Classes:
C07D499/897; A61K31/397; A61K31/47; A61K31/545; A61K31/546; A61P31/00; C07D215/56; C07D463/00; C07D477/00; C07D477/14; C07D491/06; C07D499/00; C07D499/88; C07D501/00; C07D501/34; (IPC1-7): C07D463/00; C07D477/00; C07D491/06; C07D499/88; C07D499/897; C07D501/34
Attorney, Agent or Firm:
Kazuo Sato (3 others)