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

页码：407 / 410

页数：4

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