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他氟前列素
Tier C · 观察 / 贸易Tafluprost
Santen Pharmaceutical Co Ltd
原研
2008
首批上市
-
到期年（公开口径）
$0.17B ▲
峰值销售
化学药
类型
靶点：PTGFR
商品名：Tapros、Taflotan、Zioptan
适应症（已批准）：高眼压、开角型青光眼、青光眼
各地区研发/上市状态
美国
批准上市
2012-02-10
欧盟
批准上市
2008-03-01
中国
批准上市
2015-07-27
日本
批准上市
2008-10-16
合成路线与中间体4 routes
原研路线 × 0优化路线（非专利）× 4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。
优化Route 1步骤 6 · 总收率 3.98 g
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| 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 |
优化Route 2步骤 4 · 总收率 20 mg
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| 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 | - | - |
优化Route 3步骤 7 · 总收率 6.8 g
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| 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 |
优化Route 4步骤 14 · 总收率 1.5 g
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| 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 |
常见问题（FAQ）
他氟前列素的适应症有哪些？
已批准的适应症包括：高眼压、开角型青光眼、青光眼。
他氟前列素的专利什么时候到期？
他氟前列素的专利到期年暂无公开口径，本页会在数据管道核实后更新。
他氟前列素有几条合成路线？
本站收录 4 条合成路线，最短路线 4 步、总收率 20 mg。每条路线的中间体均带登记编号与 CAS 号。
他氟前列素的关键中间体在哪里可以采购？
他氟前列素路线中的中间体均已建立 CAS 档案，可直接按 CAS 发起询价，需求会进入供应网络撮合池。
如何获取他氟前列素中间体的报价？
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