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美阿沙坦钾
Tier C · 观察 / 贸易Azilsartan Medoxomil Potassium
武田药品工业株式会社
原研
2011
首批上市
-
到期年（公开口径）
无销量数据
峰值销售
化学药
类型
靶点：AT1
商品名：Ipreziv、易达比、Edarbi
适应症（已批准）：原发性高血压、高血压
各地区研发/上市状态
美国
批准上市
2011-02-25
欧盟
批准上市
2011-12-07
中国
批准上市
2021-01-19
日本
-
合成路线与中间体7 routes
原研路线 × 1优化路线（非专利）× 6工艺路线 × 0
路线按「原研路线 → 优化路线 / 工艺路线（非专利）」排序。每条路线附本站自绘的路线流程图（中间体 → 原料药）与中间体表（编号 / CAS / 英文名），可直接用于供应商开发与询价。流程图由本站依据已授权的结构化数据自行渲染，未使用任何第三方路线图。
原研Route 1步骤 7 · 总收率 0.37 g
AZIL-001603-11-2AZIL-00221606-04-2AZIL-00357113-90-3AZIL-004114772-54-2AZIL-005139481-28-0AZIL-006136304-78-4AZIL-007139481-44-0AZIL-008147403-65-4AZIL-009147403-52-9AZIL-01091526-18-0AZIL-01180841-78-7API · 美阿沙坦钾
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| AZIL-001 | 603-11-2 | 3-nitrophthalic acid |
| AZIL-002 | 21606-04-2 | 2-(methoxycarbonyl)-6-nitrobenzoic acid |
| AZIL-003 | 57113-90-3 | methyl 2-((tert-butoxycarbonyl)amino)-3-nitrobenzoate |
| AZIL-004 | 114772-54-2 | 4'-(bromomethyl)-[1,1'-biphenyl]-2-carbonitrile |
| AZIL-005 | 139481-28-0 | methyl 2-(((2'-cyano-[1,1'-biphenyl]-4-yl)methyl)amino)-3-nitrobenzoate |
| AZIL-006 | 136304-78-4 | methyl 3-amino-2-(((2'-cyano-[1,1'-biphenyl]-4-yl)methyl)amino)benzoate |
| AZIL-007 | 139481-44-0 | methyl 1-((2'-cyano-[1,1'-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate |
| AZIL-008 | 147403-65-4 | methyl (Z)-2-ethoxy-1-((2'-(N'-hydroxycarbamimidoyl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate |
| AZIL-009 | 147403-52-9 | 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 |
| AZIL-010 | 91526-18-0 | 4-(hydroxymethyl)-5-methyl-1,3-dioxol-2-one |
| AZIL-011 | 80841-78-7 | 4-(chloromethyl)-5-methyl-1,3-dioxol-2-one |
优化Route 2步骤 9 · 总收率 0.25 g
AZIL-00357113-90-3AZIL-009147403-52-9AZIL-01239627-24-2AZIL-013147404-72-6AZIL-014147404-73-7AZIL-015147404-74-8AZIL-016147404-75-9AZIL-017147404-76-0AZIL-018147404-77-1AZIL-019—API · 美阿沙坦钾
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| AZIL-003 | 57113-90-3 | methyl 2-((tert-butoxycarbonyl)amino)-3-nitrobenzoate |
| AZIL-009 | 147403-52-9 | 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 |
| AZIL-012 | 39627-24-2 | 4'-methyl-[1,1'-biphenyl]-2-carboxamide |
| AZIL-013 | 147404-72-6 | 4'-(bromomethyl)-[1,1'-biphenyl]-2-carboxamide |
| AZIL-014 | 147404-73-7 | methyl 2-((tert-butoxycarbonyl)((2'-carbamoyl-[1,1'-biphenyl]-4-yl)methyl)amino)-3-nitrobenzoate |
| AZIL-015 | 147404-74-8 | methyl 2-(((2'-carbamoyl-[1,1'-biphenyl]-4-yl)methyl)amino)-3-nitrobenzoate |
| AZIL-016 | 147404-75-9 | methyl 3-amino-2-(((2'-carbamoyl-[1,1'-biphenyl]-4-yl)methyl)amino)benzoate |
| AZIL-017 | 147404-76-0 | methyl 1-((2'-carbamoyl-[1,1'-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate |
| AZIL-018 | 147404-77-1 | methyl 2-ethoxy-1-((2'-(ethoxy(imino)methyl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate |
| AZIL-019 | - | 2,6-dichloro-9-((3S,4R,5R)-3-fluoro-4-((triisopropylsilyl)oxy)-5-(((triisopropylsilyl)oxy)methyl)tetrahydrofuran-2-yl)-9H-purine |
优化Route 3步骤 5 · 总收率 2.9 g
AZIL-006136304-78-4AZIL-009147403-52-9AZIL-020—AZIL-021147404-81-7AZIL-022—API · 美阿沙坦钾
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| AZIL-006 | 136304-78-4 | methyl 3-amino-2-(((2'-cyano-[1,1'-biphenyl]-4-yl)methyl)amino)benzoate |
| AZIL-009 | 147403-52-9 | 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 |
| AZIL-020 | - | 2,6-dichloro-9-((3S,4R,5R)-3-fluoro-4-((triisopropylsilyl)oxy)-5-(((triisopropylsilyl)oxy)methyl)tetrahydrofuran-2-yl)-9H-purine |
| AZIL-021 | 147404-81-7 | methyl (Z)-3-amino-2-(((2'-(N'-((ethoxycarbonyl)oxy)carbamimidoyl)-[1,1'-biphenyl]-4-yl)methyl)amino)benzoate |
| AZIL-022 | - | methyl (Z)-2-ethoxy-1-((2'-(N'-((ethoxycarbonyl)oxy)carbamimidoyl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate |
优化Route 4步骤 5 · 总收率 /
AZIL-023114772-53-1AZIL-024147403-93-8AZIL-025147403-94-9AZIL-026147403-95-0AZIL-027150058-27-8AZIL-028—API · 美阿沙坦钾
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| AZIL-023 | 114772-53-1 | 4'-methyl-[1,1'-biphenyl]-2-carbonitrile |
| AZIL-024 | 147403-93-8 | N'-hydroxy-4'-methyl-[1,1'-biphenyl]-2-carboximidamide |
| AZIL-025 | 147403-94-9 | 3-(4'-methyl-[1,1'-biphenyl]-2-yl)-5-(trichloromethyl)-1,2,4-oxadiazole |
| AZIL-026 | 147403-95-0 | 3-(4'-(bromomethyl)-[1,1'-biphenyl]-2-yl)-5-(trichloromethyl)-1,2,4-oxadiazole |
| AZIL-027 | 150058-27-8 | methyl 2-ethoxy-1H-benzo[d]imidazole-7-carboxylate |
| AZIL-028 | - | 2,6-dichloro-9-((3S,4R,5R)-3-fluoro-4-((triisopropylsilyl)oxy)-5-(((triisopropylsilyl)oxy)methyl)tetrahydrofuran-2-yl)-9H-purine |
优化Route 5步骤 9 · 总收率 26.2 g
AZIL-01180841-78-7AZIL-023114772-53-1AZIL-027150058-27-8AZIL-0291627560-42-2AZIL-0301627560-43-3AZIL-031161862-33-5AZIL-0321627560-44-4AZIL-0331627560-45-5AZIL-0341627560-46-6AZIL-0351627560-47-7AZIL-0361627560-48-8API · 美阿沙坦钾
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| AZIL-011 | 80841-78-7 | 4-(chloromethyl)-5-methyl-1,3-dioxol-2-one |
| AZIL-023 | 114772-53-1 | 4'-methyl-[1,1'-biphenyl]-2-carbonitrile |
| AZIL-027 | 150058-27-8 | methyl 2-ethoxy-1H-benzo[d]imidazole-7-carboxylate |
| AZIL-029 | 1627560-42-2 | N'-hydroxy-4'-methyl-[1,1'-biphenyl]-2-carboximidamide hydrochloride |
| AZIL-030 | 1627560-43-3 | N'-((ethoxycarbonyl)oxy)-4'-methyl-[1,1'-biphenyl]-2-carboximidamide |
| AZIL-031 | 161862-33-5 | 3-(4'-methyl-[1,1'-biphenyl]-2-yl)-1,2,4-oxadiazol-5(4H)-one |
| AZIL-032 | 1627560-44-4 | tert-butyl 3-(4'-methyl-[1,1'-biphenyl]-2-yl)-5-oxo-1,2,4-oxadiazole-4(5H)-carboxylate |
| AZIL-033 | 1627560-45-5 | tert-butyl 3-(4'-(bromomethyl)-[1,1'-biphenyl]-2-yl)-5-oxo-1,2,4-oxadiazole-4(5H)-carboxylate |
| AZIL-034 | 1627560-46-6 | tert-butyl 3-(4'-((2-ethoxy-7-(methoxycarbonyl)-1H-benzo[d]imidazol-1-yl)methyl)-[1,1'-biphenyl]-2-yl)-5-oxo-1,2,4-oxadiazole-4(5H)-carboxylate |
| AZIL-035 | 1627560-47-7 | 1-((2'-(4-(tert-butoxycarbonyl)-5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylic acid |
| AZIL-036 | 1627560-48-8 | tert-butyl 3-(4'-((2-ethoxy-7-(((5-methyl-2-oxo-1,3-dioxol-4-yl)methoxy)carbonyl)-1H-benzo[d]imidazol-1-yl)methyl)-[1,1'-biphenyl]-2-yl)-5-oxo-1,2,4-oxadiazole-4(5H)-carboxylate |
优化Route 6步骤 5 · 总收率 80 g
AZIL-007139481-44-0AZIL-008147403-65-4AZIL-01180841-78-7AZIL-0371397836-49-5AZIL-038—AZIL-0397693-46-1AZIL-0401449029-80-4API · 美阿沙坦钾
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| AZIL-007 | 139481-44-0 | methyl 1-((2'-cyano-[1,1'-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate |
| AZIL-008 | 147403-65-4 | methyl (Z)-2-ethoxy-1-((2'-(N'-hydroxycarbamimidoyl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate |
| AZIL-011 | 80841-78-7 | 4-(chloromethyl)-5-methyl-1,3-dioxol-2-one |
| AZIL-037 | 1397836-49-5 | (Z)-2-ethoxy-1-((2'-(N'-hydroxycarbamimidoyl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylic acid |
| AZIL-038 | - | (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl (Z)-2-ethoxy-1-((2'-(N'-hydroxycarbamimidoyl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate |
| AZIL-039 | 7693-46-1 | 4-nitrophenyl carbonochloridate |
| AZIL-040 | 1449029-80-4 | (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl (Z)-2-ethoxy-1-((2'-(N'-(((4-nitrophenoxy)carbonyl)oxy)carbamimidoyl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate |
优化Route 7步骤 6 · 总收率 2.55 kg
AZIL-007139481-44-0AZIL-008147403-65-4AZIL-01180841-78-7AZIL-0411454372-34-9AZIL-0421454318-13-8AZIL-04474124-79-1AZIL-038—AZIL-043—API · 美阿沙坦钾
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| AZIL-007 | 139481-44-0 | methyl 1-((2'-cyano-[1,1'-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate |
| AZIL-008 | 147403-65-4 | methyl (Z)-2-ethoxy-1-((2'-(N'-hydroxycarbamimidoyl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate |
| AZIL-011 | 80841-78-7 | 4-(chloromethyl)-5-methyl-1,3-dioxol-2-one |
| AZIL-041 | 1454372-34-9 | (Z)-2-ethoxy-1-((2'-(N'-(trityloxy)carbamimidoyl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylic acid |
| AZIL-042 | 1454318-13-8 | sodium (Z)-2-ethoxy-1-((2'-(N'-(trityloxy)carbamimidoyl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate |
| AZIL-044 | 74124-79-1 | bis(2,5-dioxopyrrolidin-1-yl) carbonate |
| AZIL-038 | - | (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl (Z)-2-ethoxy-1-((2'-(N'-(trityloxy)carbamimidoyl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate |
| AZIL-043 | - | (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl (Z)-2-ethoxy-1-((2'-(N'-hydroxycarbamimidoyl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate |
常见问题（FAQ）
美阿沙坦钾的适应症有哪些？
已批准的适应症包括：原发性高血压、高血压。
美阿沙坦钾的专利什么时候到期？
美阿沙坦钾的专利到期年暂无公开口径，本页会在数据管道核实后更新。
美阿沙坦钾有几条合成路线？
本站收录 7 条合成路线，最短路线 5 步、总收率 2.9 g。每条路线的中间体均带登记编号与 CAS 号。
美阿沙坦钾的关键中间体在哪里可以采购？
美阿沙坦钾路线中的中间体均已建立 CAS 档案，可直接按 CAS 发起询价，需求会进入供应网络撮合池。
如何获取美阿沙坦钾中间体的报价？
在本页选择目标中间体的 CAS 进入档案页，或在询价页直接提交需求；CAS 会自动带入供需撮合流程，由供应网络反馈报价。
数据来源：多源数据交叉核实（仅结构化字段） · 2026-10-22