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利伐沙班
Tier A — Act nowRivaroxaban · all drugs expiring in 2026 →
拜耳
Originator
2008
First approval
2026
Expiry (public)
$7.89B ▲
Peak sales
化学药
Type
Targets：F10
Brand：拜瑞妥、Xarelto
Indications (approved)：肺栓塞、中风、先天性心脏缺损、血栓形成、静脉血栓栓塞、冠状动脉疾病、冠状动脉病变、外周动脉疾病
Regional status
US
批准上市
2011-07-01
EU
批准上市
2008-09-30
China
批准上市
2009-03-31
Japan
批准上市
2012-01-28
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 9 · Total yield 2.00%
| Code | CAS No. | Intermediate |
|---|---|---|
| RIVA-001 | 141-43-5Available | 2-aminoethan-1-ol |
| RIVA-002 | 79-04-9Available | 2-chloroacetyl chloride |
| RIVA-003 | - | 2-(2-chloroacetamido)ethyl 2-chloroacetate |
| RIVA-004 | 6320-16-7Available | 2-chloro-N-(2-hydroxyethyl)acetamide |
| RIVA-005 | 109-11-5Available | morpholin-3-one |
| RIVA-006 | 350-46-9Available | 1-fluoro-4-nitrobenzene |
| RIVA-007 | 446292-04-2Available | 4-(4-nitrophenyl)morpholin-3-one |
| RIVA-008 | 438056-69-0Available | 4-(4-aminophenyl)morpholin-3-one |
| RIVA-009 | 161596-47-0Available | (S)-2-(oxiran-2-ylmethyl)isoindoline-1,3-dione |
| RIVA-010 | 446292-07-5Available | (R)-2-(2-hydroxy-3-((4-(3-oxomorpholino)phenyl)amino)propyl)isoindoline-1,3-dione |
| RIVA-011 | 446292-08-6Available | (S)-2-((2-oxo-3-(4-(3-oxomorpholino)phenyl)oxazolidin-5-yl)methyl)isoindoline-1,3-dione |
| RIVA-012 | 1430407-73-0Available | (S)-4-(4-(5-(aminomethyl)-2-oxooxazolidin-3-yl)phenyl)morpholin-3-one oxalate |
| RIVA-013 | 42518-98-9Available | 5-chlorothiophene-2-carbonyl chloride |
OptimisedRoute 2Steps 6 · Total yield 23.7 g
| Code | CAS No. | Intermediate |
|---|---|---|
| RIVA-008 | 438056-69-0Available | 4-(4-aminophenyl)morpholin-3-one |
| RIVA-013 | 42518-98-9Available | 5-chlorothiophene-2-carbonyl chloride |
| RIVA-014 | 7283-96-7Available | 5-chlorothiophene-2-carbaldehyde |
| RIVA-015 | 24065-33-6Available | 5-chlorothiophene-2-carboxylic acid |
| RIVA-016 | 209849-99-0Available | (S)-3-aminopropane-1,2-diol hydrochloride |
| RIVA-017 | 721401-51-0Available | (S)-5-chloro-N-(2,3-dihydroxypropyl)thiophene-2-carboxamide |
| RIVA-018 | 721401-52-1Available | (S)-N-(3-bromo-2-hydroxypropyl)-5-chlorothiophene-2-carboxamide |
| RIVA-019 | 721401-53-2Available | (R)-5-chloro-N-(2-hydroxy-3-((4-(3-oxomorpholino)phenyl)amino)propyl)thiophene-2-carboxamide |
OptimisedRoute 3Steps 9 · Total yield 79 mg
| Code | CAS No. | Intermediate |
|---|---|---|
| RIVA-002 | 79-04-9Available | 2-chloroacetyl chloride |
| RIVA-007 | 446292-04-2Available | 4-(4-nitrophenyl)morpholin-3-one |
| RIVA-008 | 438056-69-0Available | 4-(4-aminophenyl)morpholin-3-one |
| RIVA-013 | 42518-98-9Available | 5-chlorothiophene-2-carbonyl chloride |
| RIVA-020 | 122-98-5Available | 2-(phenylamino)ethan-1-ol |
| RIVA-021 | 29518-11-4Available | 4-phenylmorpholin-3-one |
| RIVA-022 | 501-53-1Available | benzyl carbonochloridate |
| RIVA-023 | 1313613-18-1Available | benzyl (4-(3-oxomorpholino)phenyl)carbamate |
| RIVA-024 | 60456-26-0Available | (R)-oxiran-2-ylmethyl butyrate |
| RIVA-025 | 1117893-60-3Available | (R)-4-(4-(5-(hydroxymethyl)-2-oxooxazolidin-3-yl)phenyl)morpholin-3-one |
| RIVA-026 | 1117893-61-4Available | (R)-(2-oxo-3-(4-(3-oxomorpholino)phenyl)oxazolidin-5-yl)methyl methanesulfonate |
| RIVA-027 | 75-64-9Available | 2-methylpropan-2-amine |
| RIVA-028 | 1313613-19-2Available | (S)-4-(4-(5-((tert-butylamino)methyl)-2-oxooxazolidin-3-yl)phenyl)morpholin-3-one |
| RIVA-029 | 1313613-21-6Available | (S)-N-(tert-butyl)-5-chloro-N-((2-oxo-3-(4-(3-oxomorpholino)phenyl)oxazolidin-5-yl)methyl)thiophene-2-carboxamide |
OptimisedRoute 4Steps 5 · Total yield 3.34 g
| Code | CAS No. | Intermediate |
|---|---|---|
| RIVA-013 | 42518-98-9Available | 5-chlorothiophene-2-carbonyl chloride |
| RIVA-023 | 1313613-18-1Available | benzyl (4-(3-oxomorpholino)phenyl)carbamate |
| RIVA-030 | 67843-74-7Available | (S)-2-(chloromethyl)oxirane |
| RIVA-031 | 100-52-7Available | benzaldehyde |
| RIVA-032 | 224323-52-8Available | (S,E)-1-(benzylideneamino)-3-chloropropan-2-ol |
| RIVA-033 | 34839-13-9Available | (S)-1-amino-3-chloropropan-2-ol hydrochloride |
| RIVA-034 | 1384257-81-1Available | (S)-5-chloro-N-(3-chloro-2-hydroxypropyl)thiophene-2-carboxamide |
| RIVA-035 | - | (S)-1-chloro-3-(5-chlorothiophene-2-carboxamido)propan-2-yl acetate |
OptimisedRoute 5Steps 9 · Total yield 2.25 g
| Code | CAS No. | Intermediate |
|---|---|---|
| RIVA-008 | 438056-69-0Available | 4-(4-aminophenyl)morpholin-3-one |
| RIVA-013 | 42518-98-9Available | 5-chlorothiophene-2-carbonyl chloride |
| RIVA-025 | 1117893-60-3Available | (R)-4-(4-(5-(hydroxymethyl)-2-oxooxazolidin-3-yl)phenyl)morpholin-3-one |
| RIVA-036 | 16495-04-8Available | (S)-3-(benzyloxy)-2-hydroxypropyl 4-methylbenzenesulfonate |
| RIVA-037 | 1018979-25-3Available | (S)-1-(benzyloxy)-3-(tosyloxy)propan-2-yl acetate |
| RIVA-038 | 1447919-68-7Available | (R)-1-(benzyloxy)-3-((4-(3-oxomorpholino)phenyl)amino)propan-2-yl acetate |
| RIVA-039 | 1447919-69-8Available | (R)-1-(benzyloxy)-3-((chlorocarbonyl)(4-(3-oxomorpholino)phenyl)amino)propan-2-yl acetate |
| RIVA-040 | 1117893-59-0Available | (R)-4-(4-(5-((benzyloxy)methyl)-2-oxooxazolidin-3-yl)phenyl)morpholin-3-one |
| RIVA-041 | 1424942-80-2Available | (R)-(2-oxo-3-(4-(3-oxomorpholino)phenyl)oxazolidin-5-yl)methyl 4-methylbenzenesulfonate |
| RIVA-042 | 1424942-78-8Available | (S)-4-(4-(5-((benzylamino)methyl)-2-oxooxazolidin-3-yl)phenyl)morpholin-3-one |
| RIVA-043 | 1429333-90-3Available | (S)-N-benzyl-5-chloro-N-((2-oxo-3-(4-(3-oxomorpholino)phenyl)oxazolidin-5-yl)methyl)thiophene-2-carboxamide |
OptimisedRoute 6Steps 6 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| RIVA-008 | 438056-69-0Available | 4-(4-aminophenyl)morpholin-3-one |
| RIVA-014 | 7283-96-7Available | 5-chlorothiophene-2-carbaldehyde |
| RIVA-030 | 67843-74-7Available | (S)-2-(chloromethyl)oxirane |
| RIVA-044 | 681225-50-3Available | (S)-1-azido-3-chloropropan-2-ol |
| RIVA-045 | 127182-48-3Available | (S)-2-(azidomethyl)oxirane |
| RIVA-046 | 1429334-05-3Available | (R)-4-(4-((3-azido-2-hydroxypropyl)amino)phenyl)morpholin-3-one |
| RIVA-047 | 1349248-79-8Available | (R)-4-(4-(5-(azidomethyl)-2-oxooxazolidin-3-yl)phenyl)morpholin-3-one |
| RIVA-048 | 446292-10-0Available | (S)-4-(4-(5-(aminomethyl)-2-oxooxazolidin-3-yl)phenyl)morpholin-3-one |
Frequently asked questions
What are the approved indications of Rivaroxaban?
Approved indications include: 肺栓塞, 中风, 先天性心脏缺损, 血栓形成, 静脉血栓栓塞, 冠状动脉疾病, 冠状动脉病变, 外周动脉疾病.
When does the Rivaroxaban patent expire?
Based on public sources, the Rivaroxaban patent expires in 2026.
How many synthesis routes are recorded for Rivaroxaban?
6 synthesis routes are recorded; the shortest is 5 steps with 3.34 g total yield. Intermediates in each route carry codes and CAS numbers.
Where can I buy Rivaroxaban intermediates?
46 intermediate CAS of Rivaroxaban 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 Rivaroxaban 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