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普乐沙福有关物质的合成

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为控制普乐沙福原料药的质量,设计合成了 3个工艺杂质,分别是1,11-双[4-[(1,4,8,11-四氮杂环十四烷-1-基)甲基]苯甲基]-1,4,8,11-四氮杂环十四烷盐酸盐(有关物质A盐酸盐)、1,4-双[4-[(1,4,8,11-四氮杂环十四烷-1-基)甲基]-苯甲基]-1,4,8,11-四氮杂环十四烷盐酸盐(有关物质B盐酸盐)和1,8-双[4-[(1,4,8,11-四氮杂环十四烷-1-基)甲基]苯甲基]-1,4,8,11-四氮杂环十四烷盐酸盐(有关物质C盐酸盐),结构经1H NMR和MS确证,纯度均≥99%.该研究为普乐沙福的质量研究提供了参照品,其中有关物质A盐酸盐和B盐酸盐的合成路线为首次报道.
Synthesis of the Related Substances of Plerixafor
Three impurities of plerixafor were synthesized with the purity more than 99%,which named 1,11-bis[4-[(1,4,8,11-tetraazacyclotetradecan-1-yl)methyl]benzyl]-1,4,8,11-tetraazacyclotetradecane hydrochloride(related substance A hydrochloride),1,4-bis[4-[(1,4,8,11-tetraazacyclotetradecan-1-yl)methyl]benzyl]-1,4,8,11-tetraazacyclotetradecane hydrochloride(related substance B hydrochloride)and 1,8-bis[4-[(1,4,8,11-tetraazacyclotetradecan-1-yl)methyl]benzyl]-1,4,8,11-tetraazacyclotetradecane hydrochloride(related substance C hydrochloride),and their chemical structure were confirmed by 1H NMR and ESI-MS.The synthesis routes of the related substances A hydrochloride and B hydrochloride had been reported at the first time.They can be used as the references for the quality study of plerixafor.

plerixaforrelated substancesynthesis

赵利枝、田博、崔强、邓容、张贵民

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鲁南制药集团股份有限公司,国家手性制药工程技术研究中心,山东临沂 276005

北京沣瑞医药科技有限公司,北京 100176

普乐沙福 有关物质 合成

2024

中国医药工业杂志
上海医药工业研究院,中国化学制药工业协会

中国医药工业杂志

CSTPCD
影响因子:0.487
ISSN:1001-8255
年,卷(期):2024.55(5)
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