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CAS 603-11-2
3-nitrophthalic acid
登记编号：APER-006、AZIL-001、CAND-001、LUMI-001
应用背景（按来源药适应症）
斑块银屑病阿普米司特白塞病综合征阿普米司特口腔溃疡阿普米司特银屑病阿普米司特银屑病关节炎阿普米司特高血压阿齐沙坦酯钾盐/氯噻酮原发性高血压阿齐沙坦酯钾盐/氯噻酮高血压苯磺酸氨氯地平/坎地沙坦酯原发性高血压美阿沙坦钾高血压美阿沙坦钾高血压坎地沙坦西酯心脏衰竭坎地沙坦西酯原发性高血压坎地沙坦西酯偏头痛坎地沙坦西酯新型冠状病毒感染坎地沙坦西酯躁狂症坎地沙坦西酯免疫紊乱Luminol sodium银屑病Luminol sodium新型冠状病毒感染Luminol sodium斑块银屑病Luminol sodium
来源药（使用该中间体的合成路线）
| 品种 | 梯队 | 到期年 |
|---|---|---|
| 阿普米司特Apremilast | Tier B · 提前布局 | 2028 |
| 阿齐沙坦酯钾盐/氯噻酮Azilsartan Medoxomil Potassium/Chlorthalidone | Tier C · 观察 / 贸易 | - |
| 苯磺酸氨氯地平/坎地沙坦酯Amlodipine Besylate/Candesartan Cilexetil | Tier C · 观察 / 贸易 | - |
| 美阿沙坦钾Azilsartan Medoxomil Potassium | Tier C · 观察 / 贸易 | - |
| 坎地沙坦西酯Candesartan Cilexetil | Tier B · 提前布局 | - |
| Luminol sodium | Tier C · 观察 / 贸易 | - |
合成路线中的位置（上下游链）
按路线登记顺序排列，左→右为合成方向；高亮为当前 CAS，其余可点击跳转对应档案。
3-ethoxy-4-methoxybenzaldehyde→1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethan-1-amine→(2S)-2-acetamido-4-methylpentanoic acid→(S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethanamine (S)-2-acetamido-4-methylpentanoate→N-(1,3-dioxo-1,3-dihydroisobenzofuran-4-yl)acetamide→3-nitrophthalic acid→3-aminophthalic acid
3-ethoxy-4-methoxybenzaldehyde→1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethan-1-amine→3-nitrophthalic acid→3-ethoxy-4-methoxybenzonitrile→4-nitroisobenzofuran-1,3-dione→2-(1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl)-4-nitroisoindoline-1,3-dione→4-amino-2-(1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl)isoindoline-1,3-dione
3-nitrophthalic acid→2-(methoxycarbonyl)-6-nitrobenzoic acid→methyl 2-((tert-butoxycarbonyl)amino)-3-nitrobenzoate→4'-(bromomethyl)-[1,1'-biphenyl]-2-carbonitrile→methyl 2-(((2'-cyano-[1,1'-biphenyl]-4-yl)methyl)amino)-3-nitrobenzoate→methyl 3-amino-2-(((2'-cyano-[1,1'-biphenyl]-4-yl)methyl)amino)benzoate→methyl 1-((2'-cyano-[1,1'-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate→methyl (Z)-2-ethoxy-1-((2'-(N'-hydroxycarbamimidoyl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate→methyl 2-ethoxy-1-((2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate→4-(hydroxymethyl)-5-methyl-1,3-dioxol-2-one→4-(chloromethyl)-5-methyl-1,3-dioxol-2-one
3-nitrophthalic acid→2-(ethoxycarbonyl)-6-nitrobenzoic acid→ethyl 2-((tert-butoxycarbonyl)amino)-3-nitrobenzoate→4'-(bromomethyl)-[1,1'-biphenyl]-2-carbonitrile→ethyl 2-(((2'-cyano-[1,1'-biphenyl]-4-yl)methyl)amino)-3-nitrobenzoate→ethyl 3-amino-2-(((2'-cyano-[1,1'-biphenyl]-4-yl)methyl)amino)benzoate→triethoxymethoxyethane→ethyl 1-((2'-cyano-[1,1'-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate→ethyl 1-((2'-(1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate→1-((2'-(1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylic acid→2-ethoxy-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylic acid→cyclohexyl (1-iodoethyl) carbonate
3-nitrophthalic acid→triethoxymethoxyethane→cyclohexyl (1-iodoethyl) carbonate→1-(((cyclohexyloxy)carbonyl)oxy)ethyl 2-ethoxy-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate→2-(methoxycarbonyl)-6-nitrobenzoic acid→methyl 2-(chlorocarbonyl)-3-nitrobenzoate→methyl 2-(azidocarbonyl)-3-nitrobenzoate→methyl 2-((tert-butoxycarbonyl)amino)-3-nitrobenzoate→1-bromo-4-(bromomethyl)benzene→methyl 2-((4-bromobenzyl)(tert-butoxycarbonyl)amino)-3-nitrobenzoate→methyl 2-((4-bromobenzyl)amino)-3-nitrobenzoate→methyl 3-amino-2-((4-bromobenzyl)amino)benzoate→methyl 1-(4-bromobenzyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate→1-(4-bromobenzyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylic acid→1-(((cyclohexyloxy)carbonyl)oxy)ethyl 1-(4-bromobenzyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate→(2-(1-trityl-1H-tetrazol-5-yl)phenyl)boronic acid→benzonitrile→5-phenyl-2H-tetrazole→5-phenyl-1-trityl-1H-tetrazole
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