发明名称 |
OXIDATION PROCESS FOR PREPARING 3-FORMYL-CEPHEM DERIVATIVES |
摘要 |
<p>The present invention relates to an improved process for oxidizing 3-hydroxy-methyl-cephem derivatives to the corresponding 3-formyl-cephem derivatives. In particular this oxidation process is for the preparation of 7-[2-(5-amino-[1,2,4]thia-diazol-3-yl)-2-hydroxyimino-acetylamino]-3-formyl-8-oxo-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylic acid derivatives of formula (I) using a combination of a hypervalent iodine oxidizing agent of the type 10-I-3 such as bis(acetoxy)iodo-benzene (BAIB) and a catalyst such as 2,2,6,6-tetramethyl-1-piperidinyloxy (TEMPO). These compounds of formula (I) are intermediates in the synthesis of ceftobiprole.</p> |
申请公布号 |
EP2569321(A1) |
申请公布日期 |
2013.03.20 |
申请号 |
EP20110717676 |
申请日期 |
2011.05.09 |
申请人 |
BASILEA PHARMACEUTICA INTERNATIONAL LTD. |
发明人 |
VERVEST, IVAN, JOSEPH, MARIA |
分类号 |
C07D501/34 |
主分类号 |
C07D501/34 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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