229016-73-3Relevant articles and documents
Preparation method of ceftaroline fosamil
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Paragraph 0064-0065, (2018/09/08)
The invention belongs to the field of pharmaceutical chemistry and specifically relates to a preparation method of ceftaroline fosamil. The method includes the following steps: subjecting (Z)-2-(5-amino-1,2,4-thiadiazol-3-yl)-2-ethoxyimidoacetic acid being a raw material and halotriphenylmethane to an amidogen protecting reaction in an alkaline environment to obtain a compound represented by formula I; subjecting the compound represented by formula I and 2,4,6-trinitrofluorobenzene to a substitution reaction under alkaline condition to obtain a compound represented by formula II; subjecting the compound represented by formula II and a compound represented by formula III to an acylation reaction under alkaline condition to obtain a compound represented by formula IV; removing a triphenylmethyl group from the compound represented by formula IV under acidic condition or under catalytic hydrogenation condition to obtain a compound represented by formula V; and subjecting the compound represented by formula V and a phosphorylation reagent to a phosphorylation reaction to obtain the ceftaroline fosamil. According to the method, the obtained ceftaroline fosamil has less impurities and a high yield. The effect is significantly better than that of the prior art.
NOVEL CRYSTALLINE FORMS OF CEFTAROLINE FOSAMIL
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Page/Page column 15, (2014/07/08)
The present invention relates to novel crystalline forms of ceftaroline fosamil and to methods for their preparation. Furthermore the present invention relates to the use of the novel forms of ceftaroline fosamil for the preparation of an antibiotic medicament. In addition the present invention relates to pharmaceutical compositions comprising an effective amount of the novel forms of ceftaroline fosamil and to methods of preparing the same. Finally the present invention relates to pharmaceutical combinations comprising an effective amount of the novel forms of ceftaroline fosamil and β-lactamase inhibitors.
NOVEL PROCESS FOR PREPARING CEFTAROLINE FOSAMIL
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Page/Page column 20, (2014/05/07)
The present invention relates to a novel process for preparing ceftaroline fosamil as well as to intermediates of this process.
TAK-599, a novel N-phosphono type prodrug of anti-MRSA cephalosporin T-91825: Synthesis, physicochemical and pharmacological properties
Ishikawa, Tomoyasu,Matsunaga, Nobuyuki,Tawada, Hiroyuki,Kuroda, Noritaka,Nakayama, Yutaka,Ishibashi, Yukio,Tomimoto, Mitsumi,Ikeda, Yukihiro,Tagawa, Yoshihiko,Iizawa, Yuji,Okonogi, Kenji,Hashiguchi, Shohei,Miyake, Akio
, p. 2427 - 2437 (2007/10/03)
Crystalline 1 (TAK-599) is a novel N-phosphono prodrug of anti-methicillin-resistant Staphylococcus aureus (MRSA) cephalosporin 2a (T-91825) that has high affinity for penicillin-binding protein (PBP) 2′ (IC50; 0.90 μg/mL) and shows potent in v