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甲苯磺酸艾多沙班
Tier B · 提前布局Edoxaban Tosilate Hydrate · 2028 年到期全部品种 →
第一三共株式会社
原研
2011
首批上市
2028
到期年（公开口径）
$1.79B ▲
峰值销售
化学药
类型
靶点：F10
商品名：里先安、Lixiana/Savaysa、Lixiana、Savaysa、Roteas
适应症（已批准）：肺栓塞、静脉血栓栓塞、中风、栓塞、静脉血栓形成、缺血性卒中
各地区研发/上市状态
美国
批准上市
2015-01-08
欧盟
批准上市
2015-06-19
中国
批准上市
2018-12-25
日本
批准上市
2011-04-22
合成路线与中间体6 routes
原研路线 × 1优化路线（非专利）× 5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 13 · 总收率 7.4 g
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| EDOX-001 | 4771-80-6 | cyclohex-3-ene-1-carboxylic acid |
| EDOX-002 | 5708-19-0在售 | (S)-cyclohex-3-ene-1-carboxylic acid |
| EDOX-003 | 123536-66-3 | (1S,4S,5S)-4-iodo-6-oxabicyclo[3.2.1]octan-7-one |
| EDOX-004 | 365997-31-5 | ethyl (1S,3S,6R)-7-oxabicyclo[4.1.0]heptane-3-carboxylate |
| EDOX-005 | 365997-32-6 | ethyl (1S,3R,4R)-3-azido-4-hydroxycyclohexane-1-carboxylate |
| EDOX-006 | 365997-33-7 | ethyl (1S,3R,4R)-3-((tert-butoxycarbonyl)amino)-4-hydroxycyclohexane-1-carboxylate |
| EDOX-007 | 365997-34-8 | ethyl (1S,3R,4S)-4-azido-3-((tert-butoxycarbonyl)amino)cyclohexane-1-carboxylate |
| EDOX-008 | - | (1S,3R,4S)-4-azido-3-((tert-butoxycarbonyl)amino)cyclohexane-1-carboxylic acid |
| EDOX-009 | 480450-69-9 | tert-butyl ((1R,2S,5S)-2-azido-5-(dimethylcarbamoyl)cyclohexyl)carbamate |
| EDOX-010 | - | (1S,3R,4S)-3-amino-4-azido-N,N-dimethylcyclohexane-1-carboxamide |
| EDOX-011 | - | lithium 5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxylate |
| EDOX-012 | 480450-70-2 | N-((1R,2S,5S)-2-azido-5-(dimethylcarbamoyl)cyclohexyl)-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide |
| EDOX-013 | 480450-71-3 | N-((1R,2S,5S)-2-amino-5-(dimethylcarbamoyl)cyclohexyl)-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide |
| EDOX-014 | - | sodium 2-((5-chloropyridin-2-yl)amino)-2-oxoacetate |
优化Route 2步骤 5 · 总收率 /
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| EDOX-011 | - | lithium 5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxylate |
| EDOX-015 | 504-24-5 | pyridin-4-amine |
| EDOX-016 | 98400-69-2 | tert-butyl pyridin-4-ylcarbamate |
| EDOX-017 | 365996-04-9 | tert-butyl (3-mercaptopyridin-4-yl)carbamate |
| EDOX-018 | 273-70-1 | thiazolo[5,4-c]pyridine |
| EDOX-019 | 259809-24-0 | 5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine |
优化Route 3步骤 5 · 总收率 /
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| EDOX-011 | - | lithium 5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxylate |
| EDOX-020 | 79099-07-3 | tert-butyl 4-oxopiperidine-1-carboxylate |
| EDOX-021 | 365996-05-0 | tert-butyl 2-amino-6,7-dihydrothiazolo[5,4-c]pyridine-5(4H)-carboxylate |
| EDOX-022 | 365996-06-1 | tert-butyl 2-bromo-6,7-dihydrothiazolo[5,4-c]pyridine-5(4H)-carboxylate |
| EDOX-023 | 365996-07-2 | 2-bromo-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine |
| EDOX-024 | 143150-92-9在售 | 2-bromo-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine |
优化Route 4步骤 10 · 总收率 /
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| EDOX-011 | - | lithium 5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxylate |
| EDOX-025 | 70-23-5 | ethyl 3-bromo-2-oxopropanoate |
| EDOX-026 | 22031-64-7 | cinnamamide |
| EDOX-027 | 132629-37-9 | ethyl (E)-2-styryloxazole-4-carboxylate |
| EDOX-028 | 259809-67-1 | (E)-2-styryloxazole-4-carbaldehyde |
| EDOX-029 | 1779-49-3 | methyltriphenylphosphonium bromide |
| EDOX-030 | 259809-68-2 | (E)-2-styryl-4-vinyloxazole |
| EDOX-031 | 259809-69-3 | (E)-2-(2-styryloxazol-4-yl)ethan-1-ol |
| EDOX-032 | 259809-70-6 | (E)-2-(2-(2-styryloxazol-4-yl)ethyl)isoindoline-1,3-dione |
| EDOX-033 | 259809-71-7 | tert-butyl (E)-(2-(2-styryloxazol-4-yl)ethyl)carbamate |
| EDOX-034 | 259809-72-8 | tert-butyl (E)-2-styryl-6,7-dihydrooxazolo[5,4-c]pyridine-5(4H)-carboxylate |
| EDOX-035 | 259809-73-9 | tert-butyl 2-formyl-6,7-dihydrooxazolo[5,4-c]pyridine-5(4H)-carboxylate |
| EDOX-036 | 259809-74-0 | 5-(tert-butyl) 2-methyl 6,7-dihydrooxazolo[5,4-c]pyridine-2,5(4H)-dicarboxylate |
优化Route 5步骤 4 · 总收率 /
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| EDOX-009 | 480450-69-9 | tert-butyl ((1R,2S,5S)-2-azido-5-(dimethylcarbamoyl)cyclohexyl)carbamate |
| EDOX-011 | - | lithium 5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxylate |
| EDOX-014 | - | sodium 2-((5-chloropyridin-2-yl)amino)-2-oxoacetate |
| EDOX-037 | 365998-36-3在售 | tert-butyl ((1R,2S,5S)-2-amino-5-(dimethylcarbamoyl)cyclohexyl)carbamate |
| EDOX-038 | 480452-36-6 | tert-butyl ((1R,2S,5S)-2-(2-((5-chloropyridin-2-yl)amino)-2-oxoacetamido)-5-(dimethylcarbamoyl)cyclohexyl)carbamate |
| EDOX-039 | 482375-18-8 | N1-((1S,2R,4S)-2-amino-4-(dimethylcarbamoyl)cyclohexyl)-N2-(5-chloropyridin-2-yl)oxalamide |
优化Route 6步骤 5 · 总收率 /
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| EDOX-007 | 365997-34-8 | ethyl (1S,3R,4S)-4-azido-3-((tert-butoxycarbonyl)amino)cyclohexane-1-carboxylate |
| EDOX-037 | 365998-36-3在售 | tert-butyl ((1R,2S,5S)-2-amino-5-(dimethylcarbamoyl)cyclohexyl)carbamate |
| EDOX-040 | 480449-84-1 | ethyl (1S,3R,4S)-4-amino-3-((tert-butoxycarbonyl)amino)cyclohexane-1-carboxylate |
| EDOX-041 | 365998-33-0 | ethyl (1S,3R,4S)-4-(((benzyloxy)carbonyl)amino)-3-((tert-butoxycarbonyl)amino)cyclohexane-1-carboxylate |
| EDOX-042 | - | (1S,3R,4S)-4-(((benzyloxy)carbonyl)amino)-3-((tert-butoxycarbonyl)amino)cyclohexane-1-carboxylic acid |
| EDOX-043 | - | benzyl tert-butyl ((1S,2R,4S)-4-(dimethylcarbamoyl)cyclohexane-1,2-diyl)dicarbamate |
常见问题（FAQ）
甲苯磺酸艾多沙班的适应症有哪些？
已批准的适应症包括：肺栓塞、静脉血栓栓塞、中风、栓塞、静脉血栓形成、缺血性卒中。
甲苯磺酸艾多沙班的专利什么时候到期？
按公开口径，甲苯磺酸艾多沙班的专利到期年为 2028 年。
甲苯磺酸艾多沙班有几条合成路线？
本站收录 6 条合成路线，最短路线 4 步、总收率 /。每条路线的中间体均带登记编号与 CAS 号。
甲苯磺酸艾多沙班的关键中间体在哪里可以采购？
甲苯磺酸艾多沙班的多条路线中间体已挂接 CAS 档案，其中 3 个 CAS 已有优贝德（Unibest）供应网络在售报价，可在本页路线表中直接查看并询价。
如何获取甲苯磺酸艾多沙班中间体的报价？
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） · 2026-09-24