盐酸司来吉兰相关杂质G的合成
Synthesis of Related Impurities G of Selegiline Hydrochloride
田磊 1张维荣 2高庆 2张祖良 1王尧1
作者信息
- 1. 安徽贝克生物制药有限公司,安徽合肥 230088
- 2. 安徽贝克制药股份有限公司,安徽太和 236626
- 折叠
摘要
盐酸司来吉兰的EP标准中,杂质G为HCl同炔键加成产物(顺式Ga及反式Gb混合物),此杂质属警示结构,市售渠道无法购买,结合类似物文献合成了此杂质G(Ga、Gb)并获得了此杂质的异构体Gc(新化合物).盐酸司来吉兰制剂在做影响因素实验中的高温试验和加速稳定性试验时,会部分降解成杂质Gb及其异构体Gc.这三种杂质的合成为今后盐酸司来吉兰原料药杂质谱的研究与质量标准的建立提供了参考和依据.
Abstract
In the EP standard of selegiline hydrochloride,impurity G is the addition product of HCl homoalkyne bond(a mixture of cis Ga and trans Gb).This impurity belongs to a warning structure and cannot be purchased from the market.We synthesized this impurity G(Ga,Gb)and obtained its isomer Gc(a new compound)in combination with the analog literature.During the high temperature test and accelerated stability test in the influence factor experiment,the selegiline hydrochloride preparation will be partially degraded into the impurity Gb and its isomer Gc.The synthe-sis of these three impurities provides support and assistance for the study of the impurity profile of selegiline hydrochlo-ride and the establishment of quality standard in the future.
关键词
盐酸司来吉兰/警示结构/合成/异构体/质量标准Key words
selegiline hydrochloride/warning structure/synthesis/isomer/quality standard引用本文复制引用
出版年
2024
NETL
NSTL
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