Development of an Isolable Active Ester, Diethyl Thiophosphoryl [(Z)-(2-Aminothiazol-4-yl)-2-(Methoxyimino)acetate (DAMA) for the Synthesis of Cefotaxime

被引：1
|
作者：
Yoon, Man-Young [1 ]
Lee, Hee Bong [1 ]
Shin, Hyunik [1 ]
机构：
[1] LG Life Sci Ltd, Proc Res & Dev, Taejon 305380, South Korea
来源：
BULLETIN OF THE KOREAN CHEMICAL SOCIETY | 2011年 / 32卷 / 02期
关键词：
DAMA; Active ester; Cefotaxime; MAEM; ANTIBACTERIAL ACTIVITY; CEPHALOSPORINS;
D O I：
10.5012/bkcs.2011.32.2.407
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
An isolable activated ester, diethyl thiophosphoryl [(Z)-(2-aminothiazol-4-yl)-2-(methoxyimino)acetate (9a, DAMA) was prepared in high purity, which was at least stable for 7 d at 25 degrees C and 6 months at 5 degrees C. Its reaction with 7-ACA (4) in the presence of tributylamine in i-PrOH provided cefotaxime (1) of high purity in good yield. Preparation of DAMA and its reaction with 7-ACA (4) to 1 was performed in one-pot manner, respectively with minimal unit operations of stirring and filtration.
引用
收藏
页码：407 / 410
页数：4
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