← 返回专利悬崖列表
氟维司群
Tier B · 提前布局Fulvestrant
阿斯利康
原研
2002
首批上市
-
到期年(公开口径)
$1.03B ▲
峰值销售
化学药
类型
靶点:ERs
商品名:Faslodex、芙仕得
适应症(已批准):乳腺癌
各地区研发/上市状态
美国
批准上市
2002-04-25
欧盟
批准上市
2004-03-09
中国
批准上市
2010-06-04
日本
批准上市
2011-09-26
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 /
FULV-00155362-80-6FULV-002149051-24-1FULV-003875573-59-4FULV-0042590-41-2FULV-005875573-60-7FULV-006875573-64-1FULV-007—FULV-0081049661-87-1FULV-0091049661-86-0FULV-010—FULV-011—FULV-012148757-88-4FULV-013—FULV-014153004-31-0API · 氟维司群
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| FULV-001 | 55362-80-6 | 9-bromononan-1-ol |
| FULV-002 | 149051-24-1 | ((9-bromononyl)oxy)(tert-butyl)dimethylsilane |
| FULV-003 | 875573-59-4 | (9-((tert-butyldimethylsilyl)oxy)nonyl)magnesium bromide |
| FULV-004 | 2590-41-2 | (8R,9S,10R,13S,14S,17S)-13-methyl-3-oxo-2,3,8,9,10,11,12,13,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl acetate |
| FULV-005 | 875573-60-7 | (7R,8R,9S,10R,13S,14S,17S)-7-(9-((tert-butyldimethylsilyl)oxy)nonyl)-13-methyl-3-oxo-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl acetate |
| FULV-006 | 875573-64-1 | (7R,8R,9S,10R,13S,14S,17S)-7-(9-hydroxynonyl)-13-methyl-3-oxo-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl acetate |
| FULV-007 | - | 9-((7R,8R,9S,10R,13S,14S,17S)-17-acetoxy-13-methyl-3-oxo-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-7-yl)nonyl acetate |
| FULV-008 | 1049661-87-1 | 9-((7R,8R,9S,13S,14S,17S)-17-acetoxy-3-hydroxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-7-yl)nonyl acetate |
| FULV-009 | 1049661-86-0 | (7R,8R,9S,13S,14S,17S)-3-hydroxy-7-(9-hydroxynonyl)-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-17-yl acetate |
| FULV-010 | - | (7R,8R,9S,13S,14S,17S)-17-acetoxy-7-(9-hydroxynonyl)-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-3-yl benzoate |
| FULV-011 | - | (7R,8R,9S,13S,14S,17S)-17-acetoxy-13-methyl-7-(9-((methylsulfonyl)oxy)nonyl)-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-3-yl benzoate |
| FULV-012 | 148757-88-4 | 4,4,5,5,5-pentafluoropentane-1-thiol |
| FULV-013 | - | (7R,8R,9S,13S,14S,17S)-17-acetoxy-13-methyl-7-(9-((4,4,5,5,5-pentafluoropentyl)thio)nonyl)-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-3-yl benzoate |
| FULV-014 | 153004-31-0 | (7R,8R,9S,13S,14S,17S)-13-methyl-7-(9-((4,4,5,5,5-pentafluoropentyl)thio)nonyl)-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthrene-3,17-diol |
优化Route 2步骤 7 · 总收率 2.35 g
FULV-014153004-31-0FULV-015434-22-0FULV-016571-92-6FULV-017116-11-0FULV-018486999-08-0FULV-0194549-33-1FULV-0201107606-65-4FULV-0211107606-66-5FULV-0221107606-68-7FULV-0231107606-67-6API · 氟维司群
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| FULV-014 | 153004-31-0 | (7R,8R,9S,13S,14S,17S)-13-methyl-7-(9-((4,4,5,5,5-pentafluoropentyl)thio)nonyl)-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthrene-3,17-diol |
| FULV-015 | 434-22-0 | (8R,9S,10R,13S,14S,17S)-17-hydroxy-13-methyl-1,2,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-3H-cyclopenta[a]phenanthren-3-one |
| FULV-016 | 571-92-6 | (8R,9S,13S,14S,17S)-3,17-dihydroxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-6-one |
| FULV-017 | 116-11-0 | 2-methoxyprop-1-ene |
| FULV-018 | 486999-08-0 | (8R,9S,13S,14S,17S)-3,17-bis((2-methoxypropan-2-yl)oxy)-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-6-one |
| FULV-019 | 4549-33-1 | 1,9-dibromononane |
| FULV-020 | 1107606-65-4 | (7S,8R,9S,13S,14S,17S)-7-(9-bromononyl)-3,17-bis((2-methoxypropan-2-yl)oxy)-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-6-one |
| FULV-021 | 1107606-66-5 | (7R,8R,9S,13S,14S,17S)-7-(9-bromononyl)-3,17-bis((2-methoxypropan-2-yl)oxy)-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthrene |
| FULV-022 | 1107606-68-7 | 4,4,5,5,5-pentafluoropentyl carbamimidothioate methanesulfonate |
| FULV-023 | 1107606-67-6 | (9-((7R,8R,9S,13S,14S,17S)-3,17-bis((2-methoxypropan-2-yl)oxy)-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-7-yl)nonyl)(4,4,5,5,5-pentafluoropentyl)sulfane |
优化Route 3步骤 6 · 总收率 2.7 g
FULV-014153004-31-0FULV-024—FULV-025—FULV-026122566-22-7FULV-02753573-82-3FULV-028862700-63-8FULV-029862700-70-7API · 氟维司群
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| FULV-014 | 153004-31-0 | (7R,8R,9S,13S,14S,17S)-13-methyl-7-(9-((4,4,5,5,5-pentafluoropentyl)thio)nonyl)-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthrene-3,17-diol |
| FULV-024 | - | (8R,9S,13S,14S,17S)-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthrene-3,17-diol |
| FULV-025 | - | 2,2'-(((8R,9S,13S,14S,17S)-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthrene-3,17-diyl)bis(oxy))bis(tetrahydro-2H-pyran) |
| FULV-026 | 122566-22-7 | (8R,9S,13S,14S,17S)-13-methyl-3,17-bis((tetrahydro-2H-pyran-2-yl)oxy)-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-6-ol |
| FULV-027 | 53573-82-3 | (8R,9S,13S,14S,17S)-13-methyl-3,17-bis((tetrahydro-2H-pyran-2-yl)oxy)-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-6-one |
| FULV-028 | 862700-63-8 | (9-iodononyl)(4,4,5,5,5-pentafluoropentyl)sulfane |
| FULV-029 | 862700-70-7 | (7S,8R,9S,13S,14S,17S)-13-methyl-7-(9-((4,4,5,5,5-pentafluoropentyl)thio)nonyl)-3,17-bis((tetrahydro-2H-pyran-2-yl)oxy)-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-6-one |
优化Route 4步骤 4 · 总收率 9.0 g
FULV-014153004-31-0FULV-0194549-33-1FULV-02753573-82-3FULV-029862700-70-7FULV-0301607427-00-8FULV-031862700-61-6API · 氟维司群
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| FULV-014 | 153004-31-0 | (7R,8R,9S,13S,14S,17S)-13-methyl-7-(9-((4,4,5,5,5-pentafluoropentyl)thio)nonyl)-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthrene-3,17-diol |
| FULV-019 | 4549-33-1 | 1,9-dibromononane |
| FULV-027 | 53573-82-3 | (8R,9S,13S,14S,17S)-13-methyl-3,17-bis((tetrahydro-2H-pyran-2-yl)oxy)-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-6-one |
| FULV-029 | 862700-70-7 | (7S,8R,9S,13S,14S,17S)-13-methyl-7-(9-((4,4,5,5,5-pentafluoropentyl)thio)nonyl)-3,17-bis((tetrahydro-2H-pyran-2-yl)oxy)-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-6-one |
| FULV-030 | 1607427-00-8 | (7S,8R,9S,13S,14S,17S)-7-(9-bromononyl)-13-methyl-3,17-bis((tetrahydro-2H-pyran-2-yl)oxy)-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-6-one |
| FULV-031 | 862700-61-6 | S-(4,4,5,5,5-pentafluoropentyl) benzothioate |
优化Route 5步骤 5 · 总收率 12 g
FULV-014153004-31-0FULV-016571-92-6FULV-028862700-63-8FULV-0323434-45-5FULV-033—FULV-0341428484-17-6API · 氟维司群
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| FULV-014 | 153004-31-0 | (7R,8R,9S,13S,14S,17S)-13-methyl-7-(9-((4,4,5,5,5-pentafluoropentyl)thio)nonyl)-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthrene-3,17-diol |
| FULV-016 | 571-92-6 | (8R,9S,13S,14S,17S)-3,17-dihydroxy-13-methyl-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthren-6-one |
| FULV-028 | 862700-63-8 | (9-iodononyl)(4,4,5,5,5-pentafluoropentyl)sulfane |
| FULV-032 | 3434-45-5 | (8R,9S,13S,14S,17S)-13-methyl-6-oxo-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthrene-3,17-diyl diacetate |
| FULV-033 | - | (7S,8R,9S,13S,14S,17S)-13-methyl-6-oxo-7-(9-((4,4,5,5,5-pentafluoropentyl)thio)nonyl)-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthrene-3,17-diyl diacetate |
| FULV-034 | 1428484-17-6 | (7R,8R,9S,13S,14S,17S)-13-methyl-7-(9-((4,4,5,5,5-pentafluoropentyl)thio)nonyl)-7,8,9,11,12,13,14,15,16,17-decahydro-6H-cyclopenta[a]phenanthrene-3,17-diyl diacetate |
常见问题(FAQ)
氟维司群的适应症有哪些?
已批准的适应症包括:乳腺癌。
氟维司群的专利什么时候到期?
氟维司群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。
氟维司群有几条合成路线?
本站收录 5 条合成路线,最短路线 4 步、总收率 9.0 g。每条路线的中间体均带登记编号与 CAS 号。
氟维司群的关键中间体在哪里可以采购?
氟维司群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。
如何获取氟维司群中间体的报价?
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) · 2026-10-22