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度他雄胺
Tier B · 提前布局Dutasteride
葛兰素史克
原研
2001
首批上市
-
到期年(公开口径)
$1.35B ▲
峰值销售
化学药
类型
靶点:SRD5A
商品名:ARMADART、Avidart、Avodart、Duagen、Avolve、Yuhylyx、Zagallo、安福达
适应症(已批准):尿潴留、前列腺增生、脱发
各地区研发/上市状态
美国
批准上市
2001-11-20
欧盟
无进展
2003-03-01
中国
批准上市
2011-04-11
日本
批准上市
2009-07-07
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 5 · 总收率 /
DUTA-001302-97-6DUTA-002328-93-8DUTA-003164656-19-3DUTA-004164656-20-6DUTA-005164656-21-7DUTA-006164656-22-8DUTA-00721149-38-2API · 度他雄胺
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| DUTA-001 | 302-97-6 | (8S,9S,10R,13S,14S,17S)-10,13-dimethyl-3-oxo-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthrene-17-carboxylic acid |
| DUTA-002 | 328-93-8 | 2,5-bis(trifluoromethyl)aniline |
| DUTA-003 | 164656-19-3 | (8S,9S,10R,13S,14S,17S)-N-(2,5-bis(trifluoromethyl)phenyl)-10,13-dimethyl-3-oxo-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthrene-17-carboxamide |
| DUTA-004 | 164656-20-6 | 3-((3S,3aS,5aS,6R,9aS,9bS)-3-((2,5-bis(trifluoromethyl)phenyl)carbamoyl)-3a,6-dimethyl-7-oxododecahydro-1H-cyclopenta[a]naphthalen-6-yl)propanoic acid |
| DUTA-005 | 164656-21-7 | (4aR,4bS,6aS,7S,9aS,9bS)-N-(2,5-bis(trifluoromethyl)phenyl)-4a,6a-dimethyl-2-oxo-2,3,4,4a,4b,5,6,6a,7,8,9,9a,9b,10-tetradecahydro-1H-indeno[5,4-f]quinoline-7-carboxamide |
| DUTA-006 | 164656-22-8 | (4aR,4bS,6aS,7S,9aS,9bS,11aR)-N-(2,5-bis(trifluoromethyl)phenyl)-4a,6a-dimethyl-2-oxohexadecahydro-1H-indeno[5,4-f]quinoline-7-carboxamide |
| DUTA-007 | 21149-38-2 | 2,2,2-trifluoro-N,N-bis(trimethylsilyl)acetamide |
优化Route 2步骤 8 · 总收率 /
DUTA-001302-97-6DUTA-00876763-14-9DUTA-009103335-54-2DUTA-010103335-55-3DUTA-01173671-92-8DUTA-012103335-41-7DUTA-013104239-97-6DUTA-0142127-03-9DUTA-015103335-49-5DUTA-002328-93-8API · 度他雄胺
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| DUTA-001 | 302-97-6 | (8S,9S,10R,13S,14S,17S)-10,13-dimethyl-3-oxo-2,3,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthrene-17-carboxylic acid |
| DUTA-008 | 76763-14-9 | (3S,3aS,5aS,6R,9aS,9bS)-6-(2-carboxyethyl)-3a,6-dimethyl-7-oxododecahydro-1H-cyclopenta[a]naphthalene-3-carboxylic acid |
| DUTA-009 | 103335-54-2 | (4aR,4bS,6aS,7S,9aS,9bS)-4a,6a-dimethyl-2-oxo-2,3,4,4a,4b,5,6,6a,7,8,9,9a,9b,10-tetradecahydro-1H-indeno[5,4-f]quinoline-7-carboxylic acid |
| DUTA-010 | 103335-55-3 | (4aR,4bS,6aS,7S,9aS,9bS,11aR)-4a,6a-dimethyl-2-oxohexadecahydro-1H-indeno[5,4-f]quinoline-7-carboxylic acid |
| DUTA-011 | 73671-92-8 | methyl (4aR,4bS,6aS,7S,9aS,9bS,11aR)-4a,6a-dimethyl-2-oxohexadecahydro-1H-indeno[5,4-f]quinoline-7-carboxylate |
| DUTA-012 | 103335-41-7 | methyl (4aR,4bS,6aS,7S,9aS,9bS,11aR)-4a,6a-dimethyl-2-oxo-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-1H-indeno[5,4-f]quinoline-7-carboxylate |
| DUTA-013 | 104239-97-6 | (4aR,4bS,6aS,7S,9aS,9bS,11aR)-4a,6a-dimethyl-2-oxo-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-1H-indeno[5,4-f]quinoline-7-carboxylic acid |
| DUTA-014 | 2127-03-9 | 1,2-di(pyridin-2-yl)disulfane |
| DUTA-015 | 103335-49-5 | (4aR,4bS,6aS,7S,9aS,9bS,11aR)-S-pyridin-2-yl 4a,6a-dimethyl-2-oxo-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-1H-indeno[5,4-f]quinoline-7-carbothioate |
| DUTA-002 | 328-93-8 | 2,5-bis(trifluoromethyl)aniline |
优化Route 3步骤 3 · 总收率 22 g (Dutasteride)
DUTA-010103335-55-3DUTA-013104239-97-6DUTA-016104214-61-1DUTA-017328-92-7API · 度他雄胺
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| DUTA-010 | 103335-55-3 | (4aR,4bS,6aS,7S,9aS,9bS,11aR)-4a,6a-dimethyl-2-oxohexadecahydro-1H-indeno[5,4-f]quinoline-7-carboxylic acid |
| DUTA-013 | 104239-97-6 | (4aR,4bS,6aS,7S,9aS,9bS,11aR)-4a,6a-dimethyl-2-oxo-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-1H-indeno[5,4-f]quinoline-7-carboxylic acid |
| DUTA-016 | 104214-61-1 | (4aR,4bS,6aS,7S,9aS,9bS,11aR)-4a,6a-dimethyl-2-oxo-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-1H-indeno[5,4-f]quinoline-7-carboxamide |
| DUTA-017 | 328-92-7 | 2-iodo-1,4-bis(trifluoromethyl)benzene |
优化Route 4步骤 10 · 总收率 613 g (Dutasteride)
DUTA-01857-83-0DUTA-0193510-20-1DUTA-0201416955-18-4DUTA-02194755-24-5DUTA-02220283-95-8DUTA-02373711-89-4DUTA-010103335-55-3DUTA-0241416955-19-5DUTA-002328-93-8DUTA-006164656-22-8DUTA-0251416955-20-8API · 度他雄胺
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| DUTA-018 | 57-83-0 | (8S,9S,10R,13S,14S,17S)-17-acetyl-10,13-dimethyl-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3(2H)-one |
| DUTA-019 | 3510-20-1 | 3-((3S,3aS,5aS,6R,9aS,9bS)-3-acetyl-3a,6-dimethyl-7-oxododecahydro-1H-cyclopenta[a]naphthalen-6-yl)propanoic acid |
| DUTA-020 | 1416955-18-4 | 3-((3S,3aS,5aS,6R,9aS,9bS)-3-acetyl-3a,6-dimethyl-7-oxododecahydro-1H-cyclopenta[a]naphthalen-6-yl)propanoic (ethyl carbonic) anhydride |
| DUTA-021 | 94755-24-5 | (4aR,4bS,6aS,7S,9aS,9bS)-7-acetyl-11a-hydroxy-4a,6a-dimethylhexadecahydro-2H-indeno[5,4-f]quinolin-2-one |
| DUTA-022 | 20283-95-8 | (4aR,4bS,6aS,7S,9aS,9bS)-7-acetyl-4a,6a-dimethyl-1,3,4,4a,4b,5,6,6a,7,8,9,9a,9b,10-tetradecahydro-2H-indeno[5,4-f]quinolin-2-one |
| DUTA-023 | 73711-89-4 | (4aR,4bS,6aS,7S,9aS,9bS,11aR)-7-acetyl-4a,6a-dimethylhexadecahydro-2H-indeno[5,4-f]quinolin-2-one |
| DUTA-010 | 103335-55-3 | (4aR,4bS,6aS,7S,9aS,9bS,11aR)-4a,6a-dimethyl-2-oxohexadecahydro-1H-indeno[5,4-f]quinoline-7-carboxylic acid |
| DUTA-024 | 1416955-19-5 | (ethyl carbonic) (4aR,4bS,6aS,7S,9aS,9bS,11aR)-4a,6a-dimethyl-2-oxohexadecahydro-1H-indeno[5,4-f]quinoline-7-carboxylic anhydride |
| DUTA-002 | 328-93-8 | 2,5-bis(trifluoromethyl)aniline |
| DUTA-006 | 164656-22-8 | (4aR,4bS,6aS,7S,9aS,9bS,11aR)-N-(2,5-bis(trifluoromethyl)phenyl)-4a,6a-dimethyl-2-oxohexadecahydro-1H-indeno[5,4-f]quinoline-7-carboxamide |
| DUTA-025 | 1416955-20-8 | (3R,4aR,4bS,6aS,7S,9aS,9bS,11aR)-N-(2,5-bis(trifluoromethyl)phenyl)-3-iodo-4a,6a-dimethyl-2-oxohexadecahydro-1H-indeno[5,4-f]quinoline-7-carboxamide |
优化Route 5步骤 8 · 总收率 3.8 g (Dutasteride)
DUTA-02663-05-8DUTA-0276857-88-1DUTA-02851478-09-2DUTA-0291344087-70-2DUTA-030—DUTA-0311344087-72-4DUTA-010103335-55-3DUTA-013104239-97-6DUTA-002328-93-8API · 度他雄胺
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| DUTA-026 | 63-05-8 | (8R,9S,10R,13S,14S)-10,13-dimethyl-1,6,7,8,9,10,11,12,13,14,15,16-dodecahydro-3H-cyclopenta[a]phenanthrene-3,17(2H)-dione |
| DUTA-027 | 6857-88-1 | 3-((3aS,5aS,6R,9aR,9bS)-3a,6-dimethyl-3,7-dioxododecahydro-1H-cyclopenta[a]naphthalen-6-yl)propanoic acid |
| DUTA-028 | 51478-09-2 | (4aR,4bS,6aS,9aS,9bR)-4a,6a-dimethyl-3,4,4a,4b,5,6,6a,8,9,9a,9b,10-dodecahydro-1H-indeno[5,4-f]quinoline-2,7-dione |
| DUTA-029 | 1344087-70-2 | (4aR,4bS,6aS,7R,9aS,9bR)-7-hydroxy-4a,6a,7-trimethyl-1,3,4,4a,4b,5,6,6a,7,8,9,9a,9b,10-tetradecahydro-2H-indeno[5,4-f]quinolin-2-one |
| DUTA-030 | - | (4aR,4bS,6aS,9aS,9bS)-4a,6a,7-trimethyl-1,3,4,4a,4b,5,6,6a,9,9a,9b,10-dodecahydro-2H-indeno[5,4-f]quinolin-2-one |
| DUTA-031 | 1344087-72-4 | (4aR,4bS,6aR,7S,9aS,9bS,11aR)-4a,6a,7-trimethylhexadecahydro-2H-indeno[5,4-f]quinolin-2-one |
| DUTA-010 | 103335-55-3 | (4aR,4bS,6aS,7S,9aS,9bS,11aR)-4a,6a-dimethyl-2-oxohexadecahydro-1H-indeno[5,4-f]quinoline-7-carboxylic acid |
| DUTA-013 | 104239-97-6 | (4aR,4bS,6aS,7S,9aS,9bS,11aR)-4a,6a-dimethyl-2-oxo-2,4a,4b,5,6,6a,7,8,9,9a,9b,10,11,11a-tetradecahydro-1H-indeno[5,4-f]quinoline-7-carboxylic acid |
| DUTA-002 | 328-93-8 | 2,5-bis(trifluoromethyl)aniline |
常见问题(FAQ)
度他雄胺的适应症有哪些?
已批准的适应症包括:尿潴留、前列腺增生、脱发。
度他雄胺的专利什么时候到期?
度他雄胺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。
度他雄胺有几条合成路线?
本站收录 5 条合成路线,最短路线 3 步、总收率 22 g (Dutasteride)。每条路线的中间体均带登记编号与 CAS 号。
度他雄胺的关键中间体在哪里可以采购?
度他雄胺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。
如何获取度他雄胺中间体的报价?
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