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他氟前列素
Tier C — Watch / tradeTafluprost
Santen Pharmaceutical Co Ltd
Originator
2008
First approval
-
Expiry (public)
$0.17B ▲
Peak sales
化学药
Type
Targets：PTGFR
Brand：Tapros、Taflotan、Zioptan
Indications (approved)：高眼压、开角型青光眼、青光眼
Regional status
US
批准上市
2012-02-10
EU
批准上市
2008-03-01
China
批准上市
2015-07-27
Japan
批准上市
2008-10-16
Synthetic routes & intermediates4 routes
Originator routes × 0Optimised (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.
OptimisedRoute 1Steps 6 · Total yield 3.98 g
| Code | CAS No. | Intermediate |
|---|---|---|
| TAFL-001 | 39746-01-5 | (3aR,4R,5R,6aS)-4-formyl-2-oxohexahydro-2H-cyclopenta[b]furan-5-yl benzoate |
| TAFL-002 | 40665-68-7 | dimethyl (2-oxo-3-phenoxypropyl)phosphonate |
| TAFL-003 | 51638-91-6 | (3aR,4R,5R,6aS)-2-oxo-4-((E)-3-oxo-4-phenoxybut-1-en-1-yl)hexahydro-2H-cyclopenta[b]furan-5-yl benzoate |
| TAFL-004 | 209861-00-7 | (3aR,4R,5R,6aS)-4-((E)-3,3-difluoro-4-phenoxybut-1-en-1-yl)-2-oxohexahydro-2H-cyclopenta[b]furan-5-yl benzoate |
| TAFL-005 | 209861-02-9 | (3aR,4R,5R,6aS)-4-((E)-3,3-difluoro-4-phenoxybut-1-en-1-yl)hexahydro-2H-cyclopenta[b]furan-2,5-diol |
| TAFL-006 | 17814-85-6 | (4-carboxybutyl)triphenylphosphonium bromide |
| TAFL-007 | 209860-88-8 | (Z)-7-((1R,2R,3R,5S)-2-((E)-3,3-difluoro-4-phenoxybut-1-en-1-yl)-3,5-dihydroxycyclopentyl)hept-5-enoic acid |
| TAFL-008 | 209860-88-8 | (Z)-7-((1R,2R,3R,5S)-2-((E)-3,3-difluoro-4-phenoxybut-1-en-1-yl)-3,5-dihydroxycyclopentyl)hept-5-enoic acid |
OptimisedRoute 2Steps 4 · Total yield 20 mg
| Code | CAS No. | Intermediate |
|---|---|---|
| TAFL-009 | 1559057-77-0 | isopropyl (Z)-7-((1R,2R,3R,5S)-3,5-dihydroxy-2-((E)-3-hydroxy-4-phenoxybut-1-en-1-yl)cyclopentyl)hept-5-enoate |
| TAFL-010 | 1559057-45-2 | isopropyl (Z)-7-((1R,2R,3R,5S)-3,5-dihydroxy-2-((E)-3-oxo-4-phenoxybut-1-en-1-yl)cyclopentyl)hept-5-enoate |
| TAFL-011 | - | - |
| TAFL-012 | 1174321-08-4 | tert-butyl 5-formylpyrazine-2-carboxylate |
| TAFL-013 | - | - |
OptimisedRoute 3Steps 7 · Total yield 6.8 g
| Code | CAS No. | Intermediate |
|---|---|---|
| TAFL-018 | 1652582-59-6 | (8aR,9R,10R,11aS,Z)-9-((E)-3,3-difluoro-4-phenoxybut-1-en-1-yl)-10-hydroxy-4,5,8,8a,9,10,11,11a-octahydrocyclopenta[b]oxecin-2(3H)-one |
| TAFL-019 | 1652582-60-9 | (8aR,9R,10R,11aS,Z)-9-((E)-3,3-difluoro-4-phenoxybut-1-en-1-yl)-2-oxo-2,3,4,5,8,8a,9,10,11,11a-decahydrocyclopenta[b]oxecin-10-yl [1,1'-biphenyl]-4-carboxylate |
| TAFL-006 | 17814-85-6 | (4-carboxybutyl)triphenylphosphonium bromide |
| TAFL-007 | 209860-88-8 | (Z)-7-((1R,2R,3R,5S)-2-((E)-3,3-difluoro-4-phenoxybut-1-en-1-yl)-3,5-dihydroxycyclopentyl)hept-5-enoic acid |
| TAFL-014 | 261179-68-4 | (3aR,4R,5R,6aS)-4-((E)-3,3-difluoro-4-phenoxybut-1-en-1-yl)-5-((tetrahydro-2H-pyran-2-yl)oxy)hexahydro-2H-cyclopenta[b]furan-2-one |
| TAFL-015 | 261179-69-5 | (3aR,4R,5R,6aS)-4-((E)-3,3-difluoro-4-phenoxybut-1-en-1-yl)-5-((tetrahydro-2H-pyran-2-yl)oxy)hexahydro-2H-cyclopenta[b]furan-2-ol |
| TAFL-016 | 261179-70-8 | (Z)-7-((1R,2R,3R,5S)-2-((E)-3,3-difluoro-4-phenoxybut-1-en-1-yl)-5-hydroxy-3-((tetrahydro-2H-pyran-2-yl)oxy)cyclopentyl)hept-5-enoic acid |
| TAFL-017 | 1652582-58-5 | (8aR,9R,10R,11aS,Z)-9-((E)-3,3-difluoro-4-phenoxybut-1-en-1-yl)-10-((tetrahydro-2H-pyran-2-yl)oxy)-4,5,8,8a,9,10,11,11a-octahydrocyclopenta[b]oxecin-2(3H)-one |
OptimisedRoute 4Steps 14 · Total yield 1.5 g
| Code | CAS No. | Intermediate |
|---|---|---|
| TAFL-006 | 17814-85-6 | (4-carboxybutyl)triphenylphosphonium bromide |
| TAFL-012 | 1174321-08-4 | tert-butyl 5-formylpyrazine-2-carboxylate |
| TAFL-020 | 31752-99-5 | (3aR,4S,5R,6aS)-4-(hydroxymethyl)-2-oxohexahydro-2H-cyclopenta[b]furan-5-yl [1,1'-biphenyl]-4-carboxylate |
| TAFL-021 | 165876-61-9 | (3aR,4S,5R,6aS)-4-(((tert-butyldimethylsilyl)oxy)methyl)-2-oxohexahydro-2H-cyclopenta[b]furan-5-yl [1,1'-biphenyl]-4-carboxylate |
| TAFL-022 | 65025-94-7 | (3aR,4S,5R,6aS)-4-(((tert-butyldimethylsilyl)oxy)methyl)-5-hydroxyhexahydro-2H-cyclopenta[b]furan-2-one |
| TAFL-023 | 65025-95-8 | (3aR,4S,5R,6aS)-4-(((tert-butyldimethylsilyl)oxy)methyl)-5-((tetrahydro-2H-pyran-2-yl)oxy)hexahydro-2H-cyclopenta[b]furan-2-one |
| TAFL-024 | 197523-78-7 | (3aR,4S,5R,6aS)-4-(((tert-butyldimethylsilyl)oxy)methyl)-5-((tetrahydro-2H-pyran-2-yl)oxy)hexahydro-2H-cyclopenta[b]furan-2-ol |
| TAFL-025 | 84172-57-6 | (Z)-7-((1R,2S,3R,5S)-2-(((tert-butyldimethylsilyl)oxy)methyl)-5-hydroxy-3-((tetrahydro-2H-pyran-2-yl)oxy)cyclopentyl)hept-5-enoic acid |
| TAFL-026 | 174082-03-2 | isopropyl (Z)-7-((1R,2S,3R,5S)-2-(((tert-butyldimethylsilyl)oxy)methyl)-5-hydroxy-3-((tetrahydro-2H-pyran-2-yl)oxy)cyclopentyl)hept-5-enoate |
| TAFL-027 | 174082-04-3 | isopropyl (Z)-7-((1R,2S,3R,5S)-5-acetoxy-2-(((tert-butyldimethylsilyl)oxy)methyl)-3-((tetrahydro-2H-pyran-2-yl)oxy)cyclopentyl)hept-5-enoate |
| TAFL-028 | 174082-05-4 | isopropyl (Z)-7-((1R,2S,3R,5S)-5-acetoxy-2-(hydroxymethyl)-3-((tetrahydro-2H-pyran-2-yl)oxy)cyclopentyl)hept-5-enoate |
| TAFL-029 | 1562062-17-2 | isopropyl (Z)-7-((1R,2R,3R,5S)-5-acetoxy-2-formyl-3-((tetrahydro-2H-pyran-2-yl)oxy)cyclopentyl)hept-5-enoate |
| TAFL-030 | 40665-68-7 | dimethyl (2-oxo-3-phenoxypropyl)phosphonate |
| TAFL-031 | 1562062-19-4 | isopropyl (Z)-7-((1R,2R,3R,5S)-5-acetoxy-2-((E)-3-oxo-4-phenoxybut-1-en-1-yl)-3-((tetrahydro-2H-pyran-2-yl)oxy)cyclopentyl)hept-5-enoate |
| TAFL-032 | 1562062-22-9 | isopropyl (Z)-7-((1R,2R,3R,5S)-5-acetoxy-3-hydroxy-2-((E)-3-oxo-4-phenoxybut-1-en-1-yl)cyclopentyl)hept-5-enoate |
| TAFL-033 | 1559057-59-8 | (1R,3S,4R,5R)-4-((Z)-7-isopropoxy-7-oxohept-2-en-1-yl)-5-((E)-3-oxo-4-phenoxybut-1-en-1-yl)cyclopentane-1,3-diyl diacetate |
| TAFL-034 | 1559057-73-6 | (1S,3R,4R,5R)-4-((E)-3,3-difluoro-4-phenoxybut-1-en-1-yl)-5-((Z)-7-isopropoxy-7-oxohept-2-en-1-yl)cyclopentane-1,3-diyl diacetate |
Frequently asked questions
What are the approved indications of Tafluprost?
Approved indications include: 高眼压, 开角型青光眼, 青光眼.
When does the Tafluprost patent expire?
No public expiry year is available for Tafluprost yet; this page updates once verified.
How many synthesis routes are recorded for Tafluprost?
4 synthesis routes are recorded; the shortest is 4 steps with 20 mg total yield. Intermediates in each route carry codes and CAS numbers.
Where can I buy Tafluprost intermediates?
All intermediates in Tafluprost routes have CAS profiles — you can submit an RFQ per CAS and it enters the Unibest matching pool.
How do I get a quote for Tafluprost 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