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坎地沙坦西酯
Tier B · 提前布局Candesartan Cilexetil
阿斯利康
原研
1997
首批上市
-
到期年（公开口径）
$4.24B ▲
峰值销售
化学药
类型
靶点：AT1
商品名：Kenzen、Ratacand、Blopress、Tiadyl、Amias、Racanda、必洛斯、Atacand、Parapres
适应症（已批准）：高血压、心脏衰竭、原发性高血压
各地区研发/上市状态
美国
批准上市
1998-06-04
欧盟
批准上市
1997-04-29
中国
批准上市
2003-08-05
日本
批准上市
1999-03-12
合成路线与中间体5 routes
原研路线 × 1优化路线（非专利）× 4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 9 · 总收率 /
CAND-001603-11-2CAND-00216533-45-2CAND-003136285-65-9CAND-004114772-54-2CAND-005136285-67-1CAND-006136285-69-3CAND-00778-09-1CAND-008139481-41-7CAND-009139481-58-6CAND-010139481-59-7CAND-011139481-72-4CAND-012102672-57-1API · 坎地沙坦西酯
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| CAND-001 | 603-11-2 | 3-nitrophthalic acid |
| CAND-002 | 16533-45-2 | 2-(ethoxycarbonyl)-6-nitrobenzoic acid |
| CAND-003 | 136285-65-9 | ethyl 2-((tert-butoxycarbonyl)amino)-3-nitrobenzoate |
| CAND-004 | 114772-54-2 | 4'-(bromomethyl)-[1,1'-biphenyl]-2-carbonitrile |
| CAND-005 | 136285-67-1 | ethyl 2-(((2'-cyano-[1,1'-biphenyl]-4-yl)methyl)amino)-3-nitrobenzoate |
| CAND-006 | 136285-69-3 | ethyl 3-amino-2-(((2'-cyano-[1,1'-biphenyl]-4-yl)methyl)amino)benzoate |
| CAND-007 | 78-09-1 | triethoxymethoxyethane |
| CAND-008 | 139481-41-7 | ethyl 1-((2'-cyano-[1,1'-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate |
| CAND-009 | 139481-58-6 | ethyl 1-((2'-(1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate |
| CAND-010 | 139481-59-7 | 1-((2'-(1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylic acid |
| CAND-011 | 139481-72-4 | 2-ethoxy-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylic acid |
| CAND-012 | 102672-57-1 | cyclohexyl (1-iodoethyl) carbonate |
优化Route 2步骤 7 · 总收率 1.88 g
CAND-01357113-91-4CAND-0145337-09-7CAND-015106896-48-4CAND-0161239349-12-2CAND-017134603-82-0CAND-0181239349-13-3CAND-01999464-83-2CAND-0201239349-15-5CAND-021170791-09-0API · 坎地沙坦西酯
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| CAND-013 | 57113-91-4 | methyl 2-amino-3-nitrobenzoate |
| CAND-014 | 5337-09-7 | methyl 2-bromo-3-nitrobenzoate |
| CAND-015 | 106896-48-4 | methyl 3-amino-2-bromobenzoate |
| CAND-016 | 1239349-12-2 | methyl 2-bromo-3-((diethoxymethylene)amino)benzoate |
| CAND-017 | 134603-82-0 | (2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methanamine |
| CAND-018 | 1239349-13-3 | (E)-methyl 2-bromo-3-((ethoxy(((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)amino)methylene)amino)benzoate |
| CAND-019 | 99464-83-2 | 1-chloroethyl cyclohexyl carbonate |
| CAND-020 | 1239349-15-5 | (E)-1-(((cyclohexyloxy)carbonyl)oxy)ethyl 2-bromo-3-((ethoxy(((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)amino)methylene)amino)benzoate |
| CAND-021 | 170791-09-0 | 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 |
优化Route 3步骤 8 · 总收率 43.60 g
CAND-01999464-83-2CAND-021170791-09-0CAND-022552-16-9CAND-023606-27-9CAND-024134-20-3CAND-025856414-37-4CAND-026124750-51-2CAND-0271420806-16-1CAND-0281420806-17-2CAND-029150058-32-5API · 坎地沙坦西酯
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| CAND-019 | 99464-83-2 | 1-chloroethyl cyclohexyl carbonate |
| CAND-021 | 170791-09-0 | 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 |
| CAND-022 | 552-16-9 | 2-nitrobenzoic acid |
| CAND-023 | 606-27-9 | methyl 2-nitrobenzoate |
| CAND-024 | 134-20-3 | methyl 2-aminobenzoate |
| CAND-025 | 856414-37-4 | methyl 2-((ethoxycarbonyl)amino)-3-nitrobenzoate |
| CAND-026 | 124750-51-2 | 5-(4'-(bromomethyl)-[1,1'-biphenyl]-2-yl)-1-trityl-1H-tetrazole |
| CAND-027 | 1420806-16-1 | methyl 2-((ethoxycarbonyl)((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)amino)-3-nitrobenzoate |
| CAND-028 | 1420806-17-2 | methyl 3-amino-2-((ethoxycarbonyl)((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)amino)benzoate |
| CAND-029 | 150058-32-5 | methyl 2-ethoxy-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate |
优化Route 4步骤 15 · 总收率 2.05 g
CAND-001603-11-2CAND-00778-09-1CAND-012102672-57-1CAND-021170791-09-0CAND-03021606-04-2CAND-03173833-13-3CAND-032856414-36-3CAND-03357113-90-3CAND-034589-15-1CAND-035892505-87-2CAND-036254745-48-7CAND-037892505-89-4CAND-038892505-90-7CAND-039854538-90-2CAND-040854538-86-6CAND-041144873-97-2CAND-042100-47-0CAND-04318039-42-4CAND-044154750-11-5API · 坎地沙坦西酯
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| CAND-001 | 603-11-2 | 3-nitrophthalic acid |
| CAND-007 | 78-09-1 | triethoxymethoxyethane |
| CAND-012 | 102672-57-1 | cyclohexyl (1-iodoethyl) carbonate |
| CAND-021 | 170791-09-0 | 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 |
| CAND-030 | 21606-04-2 | 2-(methoxycarbonyl)-6-nitrobenzoic acid |
| CAND-031 | 73833-13-3 | methyl 2-(chlorocarbonyl)-3-nitrobenzoate |
| CAND-032 | 856414-36-3 | methyl 2-(azidocarbonyl)-3-nitrobenzoate |
| CAND-033 | 57113-90-3 | methyl 2-((tert-butoxycarbonyl)amino)-3-nitrobenzoate |
| CAND-034 | 589-15-1 | 1-bromo-4-(bromomethyl)benzene |
| CAND-035 | 892505-87-2 | methyl 2-((4-bromobenzyl)(tert-butoxycarbonyl)amino)-3-nitrobenzoate |
| CAND-036 | 254745-48-7 | methyl 2-((4-bromobenzyl)amino)-3-nitrobenzoate |
| CAND-037 | 892505-89-4 | methyl 3-amino-2-((4-bromobenzyl)amino)benzoate |
| CAND-038 | 892505-90-7 | methyl 1-(4-bromobenzyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate |
| CAND-039 | 854538-90-2 | 1-(4-bromobenzyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylic acid |
| CAND-040 | 854538-86-6 | 1-(((cyclohexyloxy)carbonyl)oxy)ethyl 1-(4-bromobenzyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate |
| CAND-041 | 144873-97-2 | (2-(1-trityl-1H-tetrazol-5-yl)phenyl)boronic acid |
| CAND-042 | 100-47-0 | benzonitrile |
| CAND-043 | 18039-42-4 | 5-phenyl-2H-tetrazole |
| CAND-044 | 154750-11-5 | 5-phenyl-1-trityl-1H-tetrazole |
优化Route 5步骤 12 · 总收率 36.80 mg
CAND-00778-09-1CAND-01999464-83-2CAND-03357113-90-3CAND-04318039-42-4CAND-045512182-38-6CAND-04615720-16-8CAND-0471301606-98-3CAND-0481307853-38-8CAND-0491307853-40-2CAND-0501307853-69-5CAND-0511307853-71-9CAND-0521307853-72-0CAND-0531307853-73-1CAND-0541307853-76-4CAND-0551307853-79-7CAND-056873-75-6API · 坎地沙坦西酯
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| CAND-007 | 78-09-1 | triethoxymethoxyethane |
| CAND-019 | 99464-83-2 | 1-chloroethyl cyclohexyl carbonate |
| CAND-033 | 57113-90-3 | methyl 2-((tert-butoxycarbonyl)amino)-3-nitrobenzoate |
| CAND-043 | 18039-42-4 | 5-phenyl-2H-tetrazole |
| CAND-045 | 512182-38-6 | 1-(4-methoxybenzyl)-5-phenyl-1H-tetrazole |
| CAND-046 | 15720-16-8 | 4-bromobenzyl acetate |
| CAND-047 | 1301606-98-3 | (2'-(1-(4-methoxybenzyl)-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl acetate |
| CAND-048 | 1307853-38-8 | (2'-(1-(4-methoxybenzyl)-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methanol |
| CAND-049 | 1307853-40-2 | 5-(4'-(bromomethyl)-[1,1'-biphenyl]-2-yl)-1-(4-methoxybenzyl)-1H-tetrazole |
| CAND-050 | 1307853-69-5 | methyl 2-((tert-butoxycarbonyl)((2'-(1-(4-methoxybenzyl)-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)amino)-3-nitrobenzoate |
| CAND-051 | 1307853-71-9 | methyl 2-(((2'-(1-(4-methoxybenzyl)-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)amino)-3-nitrobenzoate |
| CAND-052 | 1307853-72-0 | methyl 3-amino-2-(((2'-(1-(4-methoxybenzyl)-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)amino)benzoate |
| CAND-053 | 1307853-73-1 | methyl 2-ethoxy-1-((2'-(1-(4-methoxybenzyl)-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate |
| CAND-054 | 1307853-76-4 | 2-ethoxy-1-((2'-(1-(4-methoxybenzyl)-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylic acid |
| CAND-055 | 1307853-79-7 | 1-(((cyclohexyloxy)carbonyl)oxy)ethyl 2-ethoxy-1-((2'-(1-(4-methoxybenzyl)-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate |
| CAND-056 | 873-75-6 | (4-bromophenyl)methanol |
常见问题（FAQ）
坎地沙坦西酯的适应症有哪些？
已批准的适应症包括：高血压、心脏衰竭、原发性高血压。
坎地沙坦西酯的专利什么时候到期？
坎地沙坦西酯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。
坎地沙坦西酯有几条合成路线？
本站收录 5 条合成路线，最短路线 7 步、总收率 1.88 g。每条路线的中间体均带登记编号与 CAS 号。
坎地沙坦西酯的关键中间体在哪里可以采购？
坎地沙坦西酯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。
如何获取坎地沙坦西酯中间体的报价？
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