地拉罗司有关物质的合成

Synthesis of the related substances of deferasirox

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).