罗沙司他有关物质的合成

Synthesis of the Related Substances of Roxadustat

为控制罗沙司他的质量,制备了罗沙司他6种有关物质:4-羟基-7-苯氧基异喹啉-3-甲酸甲酯(有关物质A)、N-(4-羟基-7-苯氧基异喹啉-3-羰基)甘氨酸(有关物质B)、N-(4-羟基-7-苯氧基异喹啉-3-羰基)甘氨酸甲酯(有关物质C)、4-羟基-1-甲基-7-苯氧基异喹啉-3-甲酸(有关物质D)、4-羟基-1-甲基-7-苯氧基异喹啉-3-甲酸甲酯(有关物质E)、N-(4-羟基-1-甲基-7-苯氧基异喹啉-3-羰基)甘氨酸甲酯(有关物质F),并用质谱(MS)和核磁共振波谱(NMR)对其结构进行了确证。

In order to control the quality of roxadustat,six related substances of roxadustat were prepared:methyl 4-hydroxy-7-phenoxyisoquinoline-3-carboxylate(related substance A),N-(4-hydroxy-7-phenoxyisoquinoline-3-carbonyl)glycine(related substance B),methyl N-(4-hydroxy-7-phenoxyisoquinoline-3-carbonyl)glycinate(related substance C),4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carboxylic acid(related substance D),methyl 4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carboxylate(related substance E),methyl N-(4-hydroxy-1-methyl-7-phenoxyisoquinoline-3-carbonyl)glycinate(related substance F),and their structures were confirmed by mass spectrometry(MS)and nuclear magnetic resonance(NMR).