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采用汇聚技术生产的硼替佐米酐中有机杂质的合成与表征

Synthesis and characterization of organic impurities in bortezomib anhydride produced by a convergent technology.

作者信息

Ivanov Andrey S, Shishkov Sergey V, Zhalnina Anna A

机构信息

F-Synthesis, LLC, Posledniy Per., 11 (1), 107045 Moscow, Russia.

出版信息

Sci Pharm. 2012 Jan-Mar;80(1):67-75. doi: 10.3797/scipharm.1109-02. Epub 2011 Nov 1.

DOI:10.3797/scipharm.1109-02
PMID:22396904
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3293353/
Abstract

A profile of impurities in bortezomib anhydride, produced by a recently developed convergent technology, has been characterized. HPLC-MS analysis of the drug essence revealed three impurities: an epimer of bortezomib, resulting from partial racemization of l-phenylalanine's stereogenic center during the chemical synthesis, and two epimeric products of oxidative degradation of bortezomib, in which boron is replaced by the OH group. The impurities were obtained by chemical synthesis and characterized by physical methods.

摘要

采用最近开发的汇聚技术生产的硼替佐米酐中的杂质概况已得到表征。对药物精华进行的HPLC-MS分析揭示了三种杂质：硼替佐米的差向异构体，它是在化学合成过程中L-苯丙氨酸的手性中心部分外消旋化产生的；以及硼替佐米氧化降解的两种差向异构产物，其中硼被OH基团取代。这些杂质通过化学合成获得，并通过物理方法进行了表征。

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