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甲苯磺酸艾多沙班
Tier B — Position earlyEdoxaban Tosilate Hydrate · all drugs expiring in 2028 →
第一三共株式会社
Originator
2011
First approval
2028
Expiry (public)
$1.79B ▲
Peak sales
化学药
Type
Targets：F10
Brand：里先安、Lixiana/Savaysa、Lixiana、Savaysa、Roteas
Indications (approved)：肺栓塞、静脉血栓栓塞、中风、栓塞、静脉血栓形成、缺血性卒中
Regional status
US
批准上市
2015-01-08
EU
批准上市
2015-06-19
China
批准上市
2018-12-25
Japan
批准上市
2011-04-22
Synthetic routes & intermediates6 routes
Originator routes × 1Optimised (non-patent) × 5Process routes × 0
Routes are ordered originator first, then optimised / process (non-patent) routes; each lists steps, overall yield and the intermediate table (code / CAS / name) — ready for supplier sourcing and RFQ. Rendered by this site from structured data; no third-party route graphics used.
OriginatorRoute 1Steps 13 · Total yield 7.4 g
| Code | CAS No. | Intermediate |
|---|---|---|
| EDOX-001 | 4771-80-6 | cyclohex-3-ene-1-carboxylic acid |
| EDOX-002 | 5708-19-0Available | (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 |
OptimisedRoute 2Steps 5 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| 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 |
OptimisedRoute 3Steps 5 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| 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 | 143150-92-9Available | 2-bromo-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine |
OptimisedRoute 4Steps 10 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| 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 |
OptimisedRoute 5Steps 4 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| 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 | 365998-36-3Available | 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 |
OptimisedRoute 6Steps 5 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| EDOX-007 | 365997-34-8 | ethyl (1S,3R,4S)-4-azido-3-((tert-butoxycarbonyl)amino)cyclohexane-1-carboxylate |
| EDOX-037 | 365998-36-3Available | 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 |
Frequently asked questions
What are the approved indications of Edoxaban Tosilate Hydrate?
Approved indications include: 肺栓塞, 静脉血栓栓塞, 中风, 栓塞, 静脉血栓形成, 缺血性卒中.
When does the Edoxaban Tosilate Hydrate patent expire?
Based on public sources, the Edoxaban Tosilate Hydrate patent expires in 2028.
How many synthesis routes are recorded for Edoxaban Tosilate Hydrate?
6 synthesis routes are recorded; the shortest is 4 steps with / total yield. Intermediates in each route carry codes and CAS numbers.
Where can I buy Edoxaban Tosilate Hydrate intermediates?
3 intermediate CAS of Edoxaban Tosilate Hydrate are available through the Unibest supply network — see the route tables on this page and request a quote per CAS.
How do I get a quote for Edoxaban Tosilate Hydrate intermediates?
Open the CAS profile of the target intermediate from this page, or submit an RFQ directly — the CAS enters the matching flow automatically and the supply network responds with quotes.
Source: cross-verified data (structured fields only) · 2026-09-24