地拉罗司有关物质的合成
Synthesis of the related substances of deferasirox
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摘要: 为控制地拉罗司的药品质量,建立地拉罗司原料药的质量标准,从地拉罗司的合成路线入手,分析并合成其中可能存在的3个有关物质:2-(2-羟苯基)-4H-苯并[1,3-e]GFDA2嗪-4-酮(A)、2-羟基-N-(2-羟基苯甲酰基)-苯甲酰胺(B)、4-[3,5-二(2-羟基苯基)-1H-1,2,4-三氮唑-1-基]苯甲酸甲酯(C),并经1H NMR和MS确证结构。Abstract: To perform the quality control of deferasirox and establish its quality criterion, three related substances which were determined by analyzing the synthetic route were synthesized, and their structures were confirmed by 1H NMR and MS. These substances were 2-(2-hydroxyphenyl)-4H-benzo[1, 3-e]oxazin-4-one(A), 2-hydroxy-N-(2-hydroxyben-zoyl)-benzamide(B), and methyl-4-[3, 5-bis(2-hydroxyphenyl)- 1H- [1, 2, 4]triazol-1-yl]-benzoate(C).
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Keywords:
- deferasirox /
- related substances /
- synthesis
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[1] Wang T,Gao C,Chen BA.Deferasirox—a new oral iron chelator-review[J].J Exper Hemat(中国实验血液学杂志),2010,18(5):1359-1364. [2] Sun M,Wei HT,Shi CL,et al.Synthesis of deferasirox,an iron chelator[J].Chin New Drug J(中国新药杂志),2009,18(9):850-851. [3] Raman JV,Shah H.Process for the preparation of deferasirox:US,13988361[P].2011-11-04. [4] Rao VJ,Mukkanti K,Vekariya NA,et al.Synthesis and characterization of related substances of deferasirox,an iron(Fe3+)chelating agent[J].Synthetic Commun(合成通讯),2012,42(21):3200-3210. [5] Du DM,Chen X,Hua WT,et al.Reinvestigation on the reaction of salicylic chloride with salicylic amide and X-ray crystal structure of a new macrocyclic polyester [J].Chin J Struct Chem(结构化学),2003,22(5):512-516. [6] Xiong Y,Xia KX,Yang L,et al.Study on the facile synthesis of alkyl 4-aminobenzoate[J].J Southwest Univ(Nat Sci Ed)(西南大学学报 自然科学版),2013,35(9):74-79. [7] Furniss BS,Hannaford AJ,Smith PWG,et al.Vogel′s Text Book of Practical Organic Chemistry [M].5th Ed.Longman Scientific and Technical,1991:960-961. [8] Ye LB,Wu JY,Yang JB,et al.Synthesis of the related substances of gefitinib [J].J China Pharm Univ(中国药科大学学报),2014,45(6):667-670.
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