Isolation, Synthesis, and Characterization of Impurities and Degradants from the Clofarabine Process
Isolation, Synthesis, and Characterization of Impurities and Degradants from the Clofarabine Process
复制标题
DOI：
10.1021/op800182x
复制
发表时间：
2008-11-01
影响因子：
3.4
通讯作者：
Lovett, Dennis P.
中科院分区：
文献类型：
--
作者：
Anderson, Bruce G.;Bauta, William E.;Lovett, Dennis P.
描述了氯法拉滨工艺杂质的鉴别及其后续分离、合成和表征。发现了两种氟阿拉伯糖与氯法拉滨N-6-连接产生的同分异构体工艺杂质，还合成并表征了与工艺杂质不同的氯法拉滨碱降解产物。这些化合物由糖部分、嘌呤环或两者的修饰产生。提供了各种工艺杂质和降解产物形成的机理依据。
The identification of clofarabine process impurities and their subsequent isolation, synthesis, and characterization is described. Two isomeric process impurities resulting from N-6-attachment of a fluoroarabinose to clofarabine were found. Clofarabine's base degradation products, which were different from the process impurities, were also synthesized and characterized. These compounds resulted from modifications to the sugar moiety, the purine ring, or both. A mechanistic rationale for the formation or the various process impurities and degradation products is provided.