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Synthesis of the major isomers of Aprepitant and Fosaprepitant
Chinese Chemical Letters ( IF 9.4 ) Pub Date : 2013 , DOI: 10.1016/j.cclet.2013.07.017
Wei-Li Wan , Yun He , Mei Guan , Xiao-Long Li , Xu Cheng , Yong Wu

The synthesis of two isomers of Aprepitant (APT) and three isomers of Fosaprepitant (FPT), crucial components for quality control in manufacturing, is described. Herein, three chiral centers in the isomers of Aprepitant are established in high yield by induced crystallization and chiral reduction. Additionally, the isomers of Aprepitant are utilized to synthesize the isomers of Fosaprepitant with the same stereochemistry. All the target compounds were confirmed by elemental analyses, IR, NMR and MS data analysis.

中文翻译:

阿斯匹灵和福沙普力的主要异构体的合成

描述了Aprepitant的两种异构体(APT)和Fosaprepitant的三种异构体(FPT)的合成,这是制造过程中质量控制的关键组成部分。在此,通过诱导的结晶和手性还原,高产率地建立了阿瑞吡坦异构体中的三个手性中心。另外,阿雷替丁的异构体被用于以相同的立体化学合成福沙普雷特的异构体。所有目标化合物均通过元素分析,IR,NMR和MS数据分析确认。
更新日期:2017-01-31
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