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替格瑞洛
Tier B — Position earlyTicagrelor · all drugs expiring in 2029 →
阿斯利康
Originator
2010
First approval
2029
Expiry (public)
$1.59B ▲
Peak sales
化学药
Type
Targets：P2RY12
Brand：Brilinta、Possia、倍林达、Brilinta/Brilique、Brilique
Indications (approved)：中风、急性冠脉综合征、心肌梗塞、外周血管疾病
Regional status
US
批准上市
2011-07-20
EU
批准上市
2010-12-03
China
批准上市
2012-11-22
Japan
批准上市
2016-09-28
Synthetic routes & intermediates5 routes
Originator routes × 1Optimised (non-patent) × 4Process 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 /
| Code | CAS No. | Intermediate |
|---|---|---|
| TICA-001 | 145783-14-8Available | 4,6-dichloro-5-nitro-2-(propylthio)pyrimidine |
| TICA-002 | 155899-66-4Available | (3aR,4S,6R,6aS)-6-amino-2,2-dimethyltetrahydro-4H-cyclopenta[d][1,3]dioxol-4-ol |
| TICA-003 | 220241-59-8Available | (3aR,4S,6R,6aS)-6-((6-chloro-5-nitro-2-(propylthio)pyrimidin-4-yl)amino)-2,2-dimethyltetrahydro-4H-cyclopenta[d][1,3]dioxol-4-ol |
| TICA-004 | 220241-60-1Available | (3aR,4S,6R,6aS)-6-((5-amino-6-chloro-2-(propylthio)pyrimidin-4-yl)amino)-2,2-dimethyltetrahydro-4H-cyclopenta[d][1,3]dioxol-4-ol |
| TICA-005 | 220241-61-2Available | (3aR,4S,6R,6aS)-6-(7-chloro-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl)-2,2-dimethyltetrahydro-4H-cyclopenta[d][1,3]dioxol-4-ol |
| TICA-006 | 274693-22-0Available | (3aR,4S,6R,6aS)-6-(7-amino-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl)-2,2-dimethyltetrahydro-4H-cyclopenta[d][1,3]dioxol-4-ol |
| TICA-007 | 88016-31-3Available | methyl 2-(((trifluoromethyl)sulfonyl)oxy)acetate |
| TICA-008 | 274693-23-1Available | methyl 2-(((3aR,4S,6R,6aS)-6-(7-amino-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl)-2,2-dimethyltetrahydro-4H-cyclopenta[d][1,3]dioxol-4-yl)oxy)acetate |
| TICA-009 | 274693-24-2Available | methyl 2-(((3aR,4S,6R,6aS)-6-(7-bromo-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl)-2,2-dimethyltetrahydro-4H-cyclopenta[d][1,3]dioxol-4-yl)oxy)acetate |
| TICA-010 | 220352-38-5Available | (1R,2S)-2-(3,4-difluorophenyl)cyclopropan-1-amine |
| TICA-011 | 274693-25-3Available | methyl 2-(((3aR,4S,6R,6aS)-6-(7-(((1R,2S)-2-(3,4-difluorophenyl)cyclopropyl)amino)-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl)-2,2-dimethyltetrahydro-4H-cyclopenta[d][1,3]dioxol-4-yl)oxy)acetate |
| TICA-012 | 30472-97-0Available | potassium sodium (2R,3R)-2,3-dihydroxysuccinate |
| TICA-013 | 274693-26-4Available | 2-(((3aR,4S,6R,6aS)-6-(7-(((1R,2S)-2-(3,4-difluorophenyl)cyclopropyl)amino)-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl)-2,2-dimethyltetrahydro-4H-cyclopenta[d][1,3]dioxol-4-yl)oxy)ethan-1-ol |
| TICA-014 | 60410-16-4Available | (1R,4S)-4-hydroxycyclopent-2-en-1-yl acetate |
| TICA-015 | 51779-32-9Available | - |
| TICA-016 | 220241-57-6Available | - |
| TICA-017 | 7529-22-8Available | 4-methylmorpholine 4-oxide |
| TICA-018 | 220241-58-7Available | - |
| TICA-019 | 77-76-9Available | 2,2-dimethoxypropane |
OptimisedRoute 2Steps 9 · Total yield 19 mg
| Code | CAS No. | Intermediate |
|---|---|---|
| TICA-010 | 220352-38-5Available | (1R,2S)-2-(3,4-difluorophenyl)cyclopropan-1-amine |
| TICA-013 | 274693-26-4Available | 2-(((3aR,4S,6R,6aS)-6-(7-(((1R,2S)-2-(3,4-difluorophenyl)cyclopropyl)amino)-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl)-2,2-dimethyltetrahydro-4H-cyclopenta[d][1,3]dioxol-4-yl)oxy)ethan-1-ol |
| TICA-020 | 2171459-69-9Available | 6-hydroxy-2-thioxo-2,3-dihydropyrimidin-4(1H)-one |
| TICA-021 | 107-08-4Available | 1-iodopropane |
| TICA-022 | 145783-12-6Available | 2-(propylthio)pyrimidine-4,6-diol |
| TICA-023 | 106-49-0Available | p-toluidine |
| TICA-024 | 376608-72-9Available | (E)-2-(propylthio)-5-(p-tolyldiazenyl)pyrimidine-4,6-diol |
| TICA-025 | 376608-73-0Available | (E)-4,6-dichloro-2-(propylthio)-5-(p-tolyldiazenyl)pyrimidine |
| TICA-026 | 1415806-23-3Available | 4,6-dichloro-2-(propylthio)-5-(2-(p-tolyl)hydrazinyl)pyrimidine |
| TICA-027 | 145783-15-9Available | 4,6-dichloro-2-(propylthio)pyrimidin-5-amine |
| TICA-028 | 274693-55-9Available | 2-(((3aR,4S,6R,6aS)-6-amino-2,2-dimethyltetrahydro-4H-cyclopenta[d][1,3]dioxol-4-yl)oxy)ethan-1-ol |
| TICA-029 | 376608-74-1Available | 2-(((3aR,4S,6R,6aS)-6-((5-amino-6-chloro-2-(propylthio)pyrimidin-4-yl)amino)-2,2-dimethyltetrahydro-4H-cyclopenta[d][1,3]dioxol-4-yl)oxy)ethan-1-ol |
| TICA-030 | 376608-75-2Available | 2-(((3aR,4S,6R,6aS)-6-(7-chloro-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl)-2,2-dimethyltetrahydro-4H-cyclopenta[d][1,3]dioxol-4-yl)oxy)ethan-1-ol |
OptimisedRoute 3Steps 7 · Total yield /
| Code | CAS No. | Intermediate |
|---|---|---|
| TICA-010 | 220352-38-5Available | (1R,2S)-2-(3,4-difluorophenyl)cyclopropan-1-amine |
| TICA-031 | 34036-07-2Available | 3,4-difluorobenzaldehyde |
| TICA-032 | 141-82-2Available | malonic acid |
| TICA-033 | 112897-97-9Available | (E)-3-(3,4-difluorophenyl)acrylic acid |
| TICA-034 | 376608-66-1Available | (E)-3-(3,4-difluorophenyl)acryloyl chloride |
| TICA-035 | 89-78-1Available | (1R,2S,5R)-2-isopropyl-5-methylcyclohexan-1-ol |
| TICA-036 | 376608-67-2Available | (1R,2S,5R)-2-isopropyl-5-methylcyclohexyl (E)-3-(3,4-difluorophenyl)acrylate |
| TICA-037 | 376608-68-3Available | (1R,2S,5R)-2-isopropyl-5-methylcyclohexyl (1R,2R)-2-(3,4-difluorophenyl)cyclopropane-1-carboxylate |
| TICA-038 | 220352-36-3Available | (1R,2R)-2-(3,4-difluorophenyl)cyclopropane-1-carboxylic acid |
| TICA-039 | 378236-67-0Available | (1R,2R)-2-(3,4-difluorophenyl)cyclopropane-1-carbonyl azide |
OptimisedRoute 4Steps 5 · Total yield 192 mg
| Code | CAS No. | Intermediate |
|---|---|---|
| TICA-027 | 145783-15-9Available | 4,6-dichloro-2-(propylthio)pyrimidin-5-amine |
| TICA-040 | 1068-90-2Available | diethyl 2-acetamidomalonate |
| TICA-041 | 62-56-6Available | thiourea |
| TICA-042 | 1549834-16-3Available | sodium 5-acetamido-4,6-dihydroxypyrimidine-2-thiolate |
| TICA-043 | 133030-24-7Available | N-(4,6-dihydroxy-2-mercaptopyrimidin-5-yl)acetamide |
| TICA-044 | 106-94-5Available | 1-bromopropane |
| TICA-045 | 1549834-56-1Available | N-(4,6-dihydroxy-2-(propylthio)pyrimidin-5-yl)acetamide |
| TICA-046 | 1549834-66-3Available | 5-amino-2-(propylthio)pyrimidine-4,6-diol hydrochloride |
OptimisedRoute 5Steps 9 · Total yield 0.48 g
| Code | CAS No. | Intermediate |
|---|---|---|
| TICA-001 | 145783-14-8Available | 4,6-dichloro-5-nitro-2-(propylthio)pyrimidine |
| TICA-010 | 220352-38-5Available | (1R,2S)-2-(3,4-difluorophenyl)cyclopropan-1-amine |
| TICA-047 | 866551-95-3Available | ethyl 2-(((3aR,4S,6R,6aS)-6-(((benzyloxy)carbonyl)amino)-2,2-dimethyltetrahydro-4H-cyclopenta[d][1,3]dioxol-4-yl)oxy)acetate |
| TICA-048 | 1612796-22-1Available | ethyl 2-(((1S,2S,3S,4R)-4-(((benzyloxy)carbonyl)amino)-2,3-dihydroxycyclopentyl)oxy)acetate |
| TICA-049 | 1612796-23-2Available | ethyl 2-(((3aR,4S,6R,6aS)-6-(((benzyloxy)carbonyl)amino)-2-oxotetrahydro-4H-cyclopenta[d][1,3]dioxol-4-yl)oxy)acetate |
| TICA-050 | 1612796-24-3Available | benzyl ((3aS,4R,6S,6aR)-6-(2-hydroxyethoxy)-2-oxotetrahydro-4H-cyclopenta[d][1,3]dioxol-4-yl)carbamate |
| TICA-051 | 1612796-25-4Available | (3aS,4R,6S,6aR)-4-amino-6-(2-hydroxyethoxy)tetrahydro-4H-cyclopenta[d][1,3]dioxol-2-one |
| TICA-052 | 1612796-35-6Available | (3aS,4R,6S,6aR)-4-((6-chloro-5-nitro-2-(propylthio)pyrimidin-4-yl)amino)-6-(2-hydroxyethoxy)tetrahydro-4H-cyclopenta[d][1,3]dioxol-2-one |
| TICA-053 | 1482484-91-2Available | (3aS,4R,6S,6aR)-4-((5-amino-6-chloro-2-(propylthio)pyrimidin-4-yl)amino)-6-(2-hydroxyethoxy)tetrahydro-4H-cyclopenta[d][1,3]dioxol-2-one |
| TICA-054 | 1612796-36-7Available | (3aS,4R,6S,6aR)-4-(7-chloro-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl)-6-(2-hydroxyethoxy)tetrahydro-4H-cyclopenta[d][1,3]dioxol-2-one |
| TICA-055 | 1612796-37-8Available | (3aS,4R,6S,6aR)-4-(7-(((1R,2S)-2-(3,4-difluorophenyl)cyclopropyl)amino)-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl)-6-(2-hydroxyethoxy)tetrahydro-4H-cyclopenta[d][1,3]dioxol-2-one |
Frequently asked questions
What are the approved indications of Ticagrelor?
Approved indications include: 中风, 急性冠脉综合征, 心肌梗塞, 外周血管疾病.
When does the Ticagrelor patent expire?
Based on public sources, the Ticagrelor patent expires in 2029.
How many synthesis routes are recorded for Ticagrelor?
5 synthesis routes are recorded; the shortest is 5 steps with 192 mg total yield. Intermediates in each route carry codes and CAS numbers.
Where can I buy Ticagrelor intermediates?
55 intermediate CAS of Ticagrelor 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 Ticagrelor 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