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创新药杂质bgc1201a-r4的结构推理及确证

首发时间：2024-06-06

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刁立影（1993-），女，硕士研究生创新药研发
王晨英 ²
王晨英（1972-），男，中级工程师，博士，创新药研发

1、苏州大学药学院，江苏苏州，215000
2、博瑞生物医药（苏州）股份有限公司，江苏苏州，215000

摘要：目的探讨创新药bgc1201中未知来源的杂质bgc1201a-r4的形成原因，为后续优化工艺条件、降低杂质含量奠定基础。方法通过研究合成路线中的起始物料，排除了杂质由起始物料引入的可能性；通过比较在空气和氩气环境下进行反应的产物，确定了杂质bgc1201a-r4是bgc1201a在氧气存在下产生的氧化杂质；采用lc-ms联用技术与核磁共振技术对合成得到的纯品进行结构确认。结果确认了杂质bgc1201a-r4是bgc1201a在氧气存在下产生的氧化降解杂质。通过将工艺条件中的空气环境改为氩气保护，可以有效降低杂质在产品中的含量。根据其氧化特性，合成得到了r4含量为94%的样品，降低了杂质制备的难度，并获得了足够的r4实物，实现了杂质微量成分的核磁定性表征。结论本研究通过对合成机制的深入分析，发现杂质r4是bgc1201a的氧化降解杂质，为bgc1201生产工艺的改进及贮藏条件的确定提供了依据。

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structural inference and confirmation of the novel drug impurity

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刁立影（1993-），女，硕士研究生创新药研发
wang chenying ²
王晨英（1972-），男，中级工程师，博士，创新药研发

1、college of pharmaceutical sciences, soochow university, suzhou jiangsu, 215000, china
2、brightgene bio-medical technology co. ltd, suzhou jiangsu, 215000, china

abstract：objective the reasons for the formation of the impurity bgc1201a-r4 of unknown origin in the innovative drug bgc1201 were discussed, which laid a foundation for the subsequent optimization of process conditions and reduction of impurity content. methods by studying the starting material in the synthetic route, the possibility of impurities being introduced by the starting material was ruled out. by comparing the products of the reaction in air and argon environments, it was determined that the impurity bgc1201a-r4 is an oxidized impurity produced by bgc1201a in the presence of oxygen. lc-ms and nmr were used to confirm the structure of the synthesized products. results the impurities bgc1201a-r4 were confirmed to be oxidative degradation impurities produced by bgc1201a in the presence of oxygen. by changing the air environment in the process conditions to argon protection, the content of impurities in the product can be effectively reduced. according to its oxidation characteristics, the sample with r4 content of 94% was synthesized, which reduced the difficulty of impurity preparation, and obtained enough r4 objects to realize the nmr qualitative characterization of impurity trace components. conclusion in this study, through the in-depth analysis of the synthesis mechanism, it was found that the impurity r4 was an oxidative degradation impurity of bgc1201a, which provided a basis for the improvement of the production process of bgc1201 and the determination of storage conditions.

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刁立影，王晨英. 创新药杂质bgc1201a-r4的结构推理及确证[eb/ol]. 北京：中国科技论文在线 [2024-06-06]. https://www.paper.edu.cn/releasepaper/content/202406-17.

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创新药杂质bgc1201a-r4的结构推理及确证

论文编号	202406-17
论文题目	创新药杂质bgc1201a-r4的结构推理及确证
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