90211-01-1Relevant articles and documents
(Z) - 2 - (5- two chlorine phosphinylidynes amino -1, 2, 4-thiadiazol-3-yl) - 2-ethoxy imidogen acetyl chloride preparation method (by machine translation)
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, (2017/02/28)
The invention relates to a preparation method of (Z)-2-(5-dichlorophosphorylamino-1,2,4-thiadiazolyl-3-yl)-2-ethoxyiminoacetyl chloride. The invention discloses a preparation method of ceftaroline fosamil side chain ATDE-Cl, which comprises the following steps: oximation reaction, dehydration reaction, ammonification reaction, cyclization reaction, hydrolysis reaction and acyl-chlorination reaction. The method has the advantages of short reaction steps, accessible raw materials and high yield; and the content of the prepared ceftaroline fosamil is higher than 93%, thereby conforming to the requirements for medicinal intermediates and satisfying the demands for ceftaroline fosamil production. The preparation method is low in cost, and can create considerable economic benefits for the enterprise.
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