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芦比前列酮
Tier C · 观察 / 贸易Lubiprostone
Sucampo
原研
2006
首批上市
-
到期年（公开口径）
$0.48B ▲
峰值销售
化学药
类型
靶点：CLCN2
商品名：Amitiza
适应症（已批准）：便秘、阿片类药物引起的便秘、慢性特发性便秘
各地区研发/上市状态
美国
批准上市
2006-01-31
欧盟
无进展
2010-12-01
中国
批准上市
2023-06-27
日本
批准上市
2012-06-29
合成路线与中间体5 routes
原研路线 × 1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。
原研Route 1步骤 12 · 总收率 /
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| LUBI-001 | 118408-95-0 | (3aR,4S,5R,6aS)-5-((tetrahydro-2H-pyran-2-yl)oxy)-4-(((trimethylsilyl)oxy)methyl)hexahydro-2H-cyclopenta[b]furan-2-one |
| LUBI-002 | 69222-61-3 | (3aR,4S,5R,6aS)-4-(hydroxymethyl)-5-((tetrahydro-2H-pyran-2-yl)oxy)hexahydro-2H-cyclopenta[b]furan-2-one |
| LUBI-003 | 32233-41-3 | (3aR,4R,5R,6aS)-2-oxo-5-((tetrahydro-2H-pyran-2-yl)oxy)hexahydro-2H-cyclopenta[b]furan-4-carbaldehyde |
| LUBI-004 | 50889-46-8 | dimethyl (3,3-difluoro-2-oxoheptyl)phosphonate |
| LUBI-005 | 136790-72-2 | (3aR,4R,5R,6aS)-4-((E)-4,4-difluoro-3-oxooct-1-en-1-yl)-5-((tetrahydro-2H-pyran-2-yl)oxy)hexahydro-2H-cyclopenta[b]furan-2-one |
| LUBI-006 | 136790-73-3 | (3aR,4R,5R,6aS)-4-(4,4-difluoro-3-oxooctyl)-5-((tetrahydro-2H-pyran-2-yl)oxy)hexahydro-2H-cyclopenta[b]furan-2-one |
| LUBI-007 | 201226-21-3 | (3aR,4R,5R,6aS)-4-(4,4-difluoro-3-hydroxyoctyl)-5-((tetrahydro-2H-pyran-2-yl)oxy)hexahydro-2H-cyclopenta[b]furan-2-one |
| LUBI-008 | 201341-41-5 | (3aR,4R,5R,6aS)-4-(4,4-difluoro-3-hydroxyoctyl)-5-((tetrahydro-2H-pyran-2-yl)oxy)hexahydro-2H-cyclopenta[b]furan-2-ol |
| LUBI-009 | 50889-29-7 | (5-carboxypentyl)triphenylphosphonium bromide |
| LUBI-010 | 136790-75-5 | (Z)-7-((1R,2R,3R,5S)-2-(4,4-difluoro-3-hydroxyoctyl)-5-hydroxy-3-((tetrahydro-2H-pyran-2-yl)oxy)cyclopentyl)hept-5-enoic acid |
| LUBI-011 | 136790-77-7 | benzyl (Z)-7-((1R,2R,3R,5S)-2-(4,4-difluoro-3-hydroxyoctyl)-5-hydroxy-3-((tetrahydro-2H-pyran-2-yl)oxy)cyclopentyl)hept-5-enoate |
| LUBI-012 | 136790-78-8 | benzyl (Z)-7-((1R,2R,3R)-2-(4,4-difluoro-3-oxooctyl)-5-oxo-3-((tetrahydro-2H-pyran-2-yl)oxy)cyclopentyl)hept-5-enoate |
| LUBI-013 | 136790-79-9 | benzyl (Z)-7-((1R,2R,3R)-2-(4,4-difluoro-3-oxooctyl)-3-hydroxy-5-oxocyclopentyl)hept-5-enoate |
| LUBI-014 | 136790-76-6 | 7-((1R,2R,3R)-2-(4,4-difluoro-3-oxooctyl)-3-hydroxy-5-oxocyclopentyl)heptanoic acid |
优化Route 2步骤 11 · 总收率 /
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| LUBI-004 | 50889-46-8 | dimethyl (3,3-difluoro-2-oxoheptyl)phosphonate |
| LUBI-010 | 136790-75-5 | (Z)-7-((1R,2R,3R,5S)-2-(4,4-difluoro-3-hydroxyoctyl)-5-hydroxy-3-((tetrahydro-2H-pyran-2-yl)oxy)cyclopentyl)hept-5-enoic acid |
| LUBI-015 | - | (3aR,4S,5R,6aS)-2-oxo-4-(((trimethylsilyl)oxy)methyl)hexahydro-2H-cyclopenta[b]furan-5-yl [1,1'-biphenyl]-4-carboxylate |
| LUBI-016 | 31752-99-5 | (3aR,4S,5R,6aS)-4-(hydroxymethyl)-2-oxohexahydro-2H-cyclopenta[b]furan-5-yl [1,1'-biphenyl]-4-carboxylate |
| LUBI-017 | 38754-71-1 | (3aR,4R,5R,6aS)-4-formyl-2-oxohexahydro-2H-cyclopenta[b]furan-5-yl [1,1'-biphenyl]-4-carboxylate |
| LUBI-018 | - | (3aR,4R,5R,6aS)-4-((E)-4,4-difluoro-3-oxooct-1-en-1-yl)-2-oxohexahydro-2H-cyclopenta[b]furan-5-yl [1,1'-biphenyl]-4-carboxylate |
| LUBI-019 | - | (3aR,4R,5R,6aS)-4-(4,4-difluoro-3-oxooctyl)-2-oxohexahydro-2H-cyclopenta[b]furan-5-yl [1,1'-biphenyl]-4-carboxylate |
| LUBI-020 | - | (3aR,4R,5R,6aS)-4-(4,4-difluoro-3-hydroxyoctyl)-2-oxohexahydro-2H-cyclopenta[b]furan-5-yl [1,1'-biphenyl]-4-carboxylate |
| LUBI-021 | - | (3aR,4R,5R,6aS)-4-(3-((tert-butyldimethylsilyl)oxy)-4,4-difluorooctyl)-2-oxohexahydro-2H-cyclopenta[b]furan-5-yl [1,1'-biphenyl]-4-carboxylate |
| LUBI-022 | 201226-28-0 | (3aR,4R,5R,6aS)-4-(3-((tert-butyldimethylsilyl)oxy)-4,4-difluorooctyl)-5-((tetrahydro-2H-pyran-2-yl)oxy)hexahydro-2H-cyclopenta[b]furan-2-one |
| LUBI-023 | 201341-43-7 | (3aR,4R,5R,6aS)-4-(3-((tert-butyldimethylsilyl)oxy)-4,4-difluorooctyl)-5-((tetrahydro-2H-pyran-2-yl)oxy)hexahydro-2H-cyclopenta[b]furan-2-ol |
| LUBI-024 | 148999-69-3 | (6-methoxy-6-oxohexyl)triphenylphosphonium bromide |
| LUBI-025 | 118583-11-2 | methyl (Z)-7-((1R,2R,3R,5S)-2-(3-((tert-butyldimethylsilyl)oxy)-4,4-difluorooctyl)-5-hydroxy-3-((tetrahydro-2H-pyran-2-yl)oxy)cyclopentyl)hept-5-enoate |
| LUBI-026 | 118583-12-3 | methyl (Z)-7-((1R,2R,3R,5S)-2-(4,4-difluoro-3-hydroxyoctyl)-5-hydroxy-3-((tetrahydro-2H-pyran-2-yl)oxy)cyclopentyl)hept-5-enoate |
优化Route 3步骤 11 · 总收率 0.32 g
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| LUBI-027 | 667-27-6 | ethyl 2-bromo-2,2-difluoroacetate |
| LUBI-028 | 123-72-8 | butyraldehyde |
| LUBI-029 | 181825-79-6 | ethyl 2,2-difluoro-3-hydroxyhexanoate |
| LUBI-030 | 1346523-54-3 | ethyl (E)-2,2-difluorohex-3-enoate |
| LUBI-031 | 1372609-18-1 | (E)-4,4-difluoro-1-(trimethylsilyl)oct-5-en-1-yn-3-one |
| LUBI-032 | 1372609-19-2 | (E)-4,4-difluorooct-5-en-1-yn-3-ol |
| LUBI-033 | 1372609-22-7 | (1E,5E)-4,4-difluoro-1-(tributylstannyl)octa-1,5-dien-3-ol |
| LUBI-034 | 1372609-23-8 | tributyl((1E,5E)-4,4-difluoro-3-((4-methoxybenzyl)oxy)octa-1,5-dien-1-yl)stannane |
| LUBI-035 | 474944-36-0 | isopropyl (R,Z)-7-(3-((tert-butyldimethylsilyl)oxy)-5-oxocyclopent-1-en-1-yl)hept-5-enoate |
| LUBI-036 | 1372609-25-0 | isopropyl (Z)-7-((1R,2R,3R)-3-((tert-butyldimethylsilyl)oxy)-2-((1E,5E)-4,4-difluoro-3-((4-methoxybenzyl)oxy)octa-1,5-dien-1-yl)-5-oxocyclopentyl)hept-5-enoate |
| LUBI-037 | 1372609-14-7 | isopropyl 7-((1R,2R,3R)-3-((tert-butyldimethylsilyl)oxy)-2-(4,4-difluoro-3-hydroxyoctyl)-5-oxocyclopentyl)heptanoate |
| LUBI-038 | 1372609-15-8 | isopropyl 7-((1R,2R,3R)-3-((tert-butyldimethylsilyl)oxy)-2-(4,4-difluoro-3-oxooctyl)-5-oxocyclopentyl)heptanoate |
| LUBI-039 | 1372609-16-9 | 7-((1R,2R,3R)-3-((tert-butyldimethylsilyl)oxy)-2-(4,4-difluoro-3-oxooctyl)-5-oxocyclopentyl)heptanoic acid |
优化Route 4步骤 9 · 总收率 /
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| LUBI-004 | 50889-46-8 | dimethyl (3,3-difluoro-2-oxoheptyl)phosphonate |
| LUBI-009 | 50889-29-7 | (5-carboxypentyl)triphenylphosphonium bromide |
| LUBI-040 | 32233-40-2 | (3aR,4S,5R,6aS)-5-hydroxy-4-(hydroxymethyl)hexahydro-2H-cyclopenta[b]furan-2-one |
| LUBI-041 | 65025-94-7 | (3aR,4S,5R,6aS)-4-(((tert-butyldimethylsilyl)oxy)methyl)-5-hydroxyhexahydro-2H-cyclopenta[b]furan-2-one |
| LUBI-042 | 1384885-37-3 | (3aR,4S,5R,6aS)-4-(((tert-butyldimethylsilyl)oxy)methyl)-5-((4-methoxybenzyl)oxy)hexahydro-2H-cyclopenta[b]furan-2-one |
| LUBI-043 | 1384885-25-9 | (3aR,4S,5R,6aS)-4-(((tert-butyldimethylsilyl)oxy)methyl)-5-((4-methoxybenzyl)oxy)hexahydro-2H-cyclopenta[b]furan-2-ol |
| LUBI-044 | 1384885-27-1 | (Z)-7-((1R,2S,3R,5S)-2-(((tert-butyldimethylsilyl)oxy)methyl)-5-hydroxy-3-((4-methoxybenzyl)oxy)cyclopentyl)hept-5-enoic acid |
| LUBI-045 | 1431770-99-8 | benzyl (Z)-7-((1R,2S,3R,5S)-2-(((tert-butyldimethylsilyl)oxy)methyl)-5-hydroxy-3-((4-methoxybenzyl)oxy)cyclopentyl)hept-5-enoate |
| LUBI-046 | 1210039-39-6 | benzyl (Z)-7-((1R,2S,3R,5S)-5-hydroxy-2-(hydroxymethyl)-3-((4-methoxybenzyl)oxy)cyclopentyl)hept-5-enoate |
| LUBI-047 | - | benzyl (Z)-7-((1R,2R,3R,5S)-2-formyl-5-hydroxy-3-((4-methoxybenzyl)oxy)cyclopentyl)hept-5-enoate |
| LUBI-048 | 1210039-41-0 | benzyl (Z)-7-((1R,2R,3R)-2-((E)-4,4-difluoro-3-oxooct-1-en-1-yl)-3-((4-methoxybenzyl)oxy)-5-oxocyclopentyl)hept-5-enoate |
优化Route 5步骤 8 · 总收率 4.1 g
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| LUBI-004 | 50889-46-8 | dimethyl (3,3-difluoro-2-oxoheptyl)phosphonate |
| LUBI-009 | 50889-29-7 | (5-carboxypentyl)triphenylphosphonium bromide |
| LUBI-040 | 32233-40-2 | (3aR,4S,5R,6aS)-5-hydroxy-4-(hydroxymethyl)hexahydro-2H-cyclopenta[b]furan-2-one |
| LUBI-046 | 1210039-39-6 | benzyl (Z)-7-((1R,2S,3R,5S)-5-hydroxy-2-(hydroxymethyl)-3-((4-methoxybenzyl)oxy)cyclopentyl)hept-5-enoate |
| LUBI-048 | 1210039-41-0 | benzyl (Z)-7-((1R,2R,3R)-2-((E)-4,4-difluoro-3-oxooct-1-en-1-yl)-3-((4-methoxybenzyl)oxy)-5-oxocyclopentyl)hept-5-enoate |
| LUBI-049 | 39746-00-4 | (3aR,4S,5R,6aS)-4-(hydroxymethyl)-2-oxohexahydro-2H-cyclopenta[b]furan-5-yl benzoate |
| LUBI-050 | 2186-92-7 | 1-(dimethoxymethyl)-4-methoxybenzene |
| LUBI-051 | 1210039-33-0 | (4aS,4bR,7aS,8aR)-2-(4-methoxyphenyl)hexahydrofuro[3',2':3,4]cyclopenta[1,2-d][1,3]dioxin-6(4H)-one |
| LUBI-052 | 1210039-35-2 | (3aR,4S,5R,6aS)-4-(hydroxymethyl)-5-((4-methoxybenzyl)oxy)hexahydro-2H-cyclopenta[b]furan-2-ol |
| LUBI-053 | 1210039-37-4 | (Z)-7-((1R,2S,3R,5S)-5-hydroxy-2-(hydroxymethyl)-3-((4-methoxybenzyl)oxy)cyclopentyl)hept-5-enoic acid |
| LUBI-054 | 1210039-40-9 | benzyl (Z)-7-((1R,2R,3R)-2-formyl-3-((4-methoxybenzyl)oxy)-5-oxocyclopentyl)hept-5-enoate |
常见问题（FAQ）
芦比前列酮的适应症有哪些？
已批准的适应症包括：便秘、阿片类药物引起的便秘、慢性特发性便秘。
芦比前列酮的专利什么时候到期？
芦比前列酮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。
芦比前列酮有几条合成路线？
本站收录 5 条合成路线，最短路线 8 步、总收率 4.1 g。每条路线的中间体均带登记编号与 CAS 号。
芦比前列酮的关键中间体在哪里可以采购？
芦比前列酮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。
如何获取芦比前列酮中间体的报价？
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