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赛洛多辛
Tier C · 观察 / 贸易Silodosin
橘生药品工业株式会社
原研
2006
首批上市
-
到期年（公开口径）
$0.38B ▲
峰值销售
化学药
类型
靶点：ADRA1
商品名：Rapaflo、Urorec、优利福、Silodyx、Urief
适应症（已批准）：前列腺增生
各地区研发/上市状态
美国
撤市
欧盟
批准上市
2010-01-29
中国
批准上市
2011-08-25
日本
批准上市
2006-01-23
合成路线与中间体5 routes
原研路线 × 1优化路线（非专利）× 3工艺路线 × 1
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 18 · 总收率 /
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| SILO-001 | 160968-91-2 | 1-(1-acetylindolin-5-yl)propan-1-one |
| SILO-002 | 175837-02-2 | 1-(1-acetylindolin-5-yl)-2-bromopropan-1-one |
| SILO-003 | 160968-93-4 | 1-(5-(2-bromopropyl)indolin-1-yl)ethan-1-one |
| SILO-004 | 160968-94-5 | 1-(5-(2-bromopropyl)-7-nitroindolin-1-yl)ethan-1-one |
| SILO-005 | 160968-95-6 | 1-(7-amino-5-(2-bromopropyl)indolin-1-yl)ethan-1-one |
| SILO-006 | 160968-96-7 | 1-acetyl-5-(2-bromopropyl)indoline-7-carbonitrile |
| SILO-007 | 160968-97-8 | 1-acetyl-5-(2-azidopropyl)indoline-7-carbonitrile |
| SILO-008 | 175837-01-1 | 1-acetyl-5-(2-aminopropyl)indoline-7-carbonitrile |
| SILO-009 | 160969-00-6 | 1-(2-bromoethoxy)-2-(2,2,2-trifluoroethoxy)benzene |
| SILO-010 | 175837-07-7 | 1-acetyl-5-(2-((2-(2-(2,2,2-trifluoroethoxy)phenoxy)ethyl)amino)propyl)indoline-7-carbonitrile |
| SILO-011 | 161024-53-9 | (R)-1-acetyl-5-(2-((2-(2-(2,2,2-trifluoroethoxy)phenoxy)ethyl)amino)propyl)indoline-7-carbonitrile |
| SILO-012 | 160969-12-0 | tert-butyl (R)-(1-(1-acetyl-7-cyanoindolin-5-yl)propan-2-yl)(2-(2-(2,2,2-trifluoroethoxy)phenoxy)ethyl)carbamate |
| SILO-013 | 160969-20-0 | tert-butyl (R)-(1-(7-cyanoindolin-5-yl)propan-2-yl)(2-(2-(2,2,2-trifluoroethoxy)phenoxy)ethyl)carbamate |
| SILO-014 | 160969-27-7 | tert-butyl (R)-(1-(7-carbamoylindolin-5-yl)propan-2-yl)(2-(2-(2,2,2-trifluoroethoxy)phenoxy)ethyl)carbamate |
| SILO-015 | - | 3-((tert-butyldimethylsilyl)oxy)propyl 4-nitrobenzenesulfonate |
| SILO-016 | 160970-01-4 | tert-butyl (R)-(1-(1-(3-((tert-butyldimethylsilyl)oxy)propyl)-7-carbamoylindolin-5-yl)propan-2-yl)(2-(2-(2,2,2-trifluoroethoxy)phenoxy)ethyl)carbamate |
| SILO-017 | 160970-07-0 | tert-butyl (R)-(1-(7-carbamoyl-1-(3-hydroxypropyl)indolin-5-yl)propan-2-yl)(2-(2-(2,2,2-trifluoroethoxy)phenoxy)ethyl)carbamate |
| SILO-018 | 90-05-1 | 2-methoxyphenol |
| SILO-019 | 353-83-3 | 1,1,1-trifluoro-2-iodoethane |
| SILO-020 | 106854-74-4 | 1-methoxy-2-(2,2,2-trifluoroethoxy)benzene |
| SILO-021 | 160968-99-0 | 2-(2,2,2-trifluoroethoxy)phenol |
| SILO-022 | 106-93-4在售 | 1,2-dibromoethane |
优化Route 2步骤 7 · 总收率 /
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| SILO-018 | 90-05-1 | 2-methoxyphenol |
| SILO-019 | 353-83-3 | 1,1,1-trifluoro-2-iodoethane |
| SILO-020 | 106854-74-4 | 1-methoxy-2-(2,2,2-trifluoroethoxy)benzene |
| SILO-021 | 160968-99-0 | 2-(2,2,2-trifluoroethoxy)phenol |
| SILO-023 | 4360-63-8 | 2-(bromomethyl)-1,3-dioxolane |
| SILO-024 | 1269801-74-2 | 2-((2-(2,2,2-trifluoroethoxy)phenoxy)methyl)-1,3-dioxolane |
| SILO-025 | 1269801-73-1 | 2-(2-(2,2,2-trifluoroethoxy)phenoxy)acetaldehyde |
| SILO-026 | 239463-72-0 | (R)-3-(5-(2-aminopropyl)-7-cyanoindolin-1-yl)propyl benzoate |
| SILO-027 | 885340-11-4 | (R)-3-(7-cyano-5-(2-((2-(2-(2,2,2-trifluoroethoxy)phenoxy)ethyl)amino)propyl)indolin-1-yl)propyl benzoate |
| SILO-028 | 885340-13-6 | (R)-1-(3-hydroxypropyl)-5-(2-((2-(2-(2,2,2-trifluoroethoxy)phenoxy)ethyl)amino)propyl)indoline-7-carbonitrile |
优化Route 3步骤 12 · 总收率 35 g
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| SILO-026 | 239463-72-0 | (R)-3-(5-(2-aminopropyl)-7-cyanoindolin-1-yl)propyl benzoate |
| SILO-027 | 885340-11-4 | (R)-3-(7-cyano-5-(2-((2-(2-(2,2,2-trifluoroethoxy)phenoxy)ethyl)amino)propyl)indolin-1-yl)propyl benzoate |
| SILO-028 | 885340-13-6 | (R)-1-(3-hydroxypropyl)-5-(2-((2-(2-(2,2,2-trifluoroethoxy)phenoxy)ethyl)amino)propyl)indoline-7-carbonitrile |
| SILO-029 | 496-15-1 | indoline |
| SILO-030 | 942-95-0 | 3-chloropropyl benzoate |
| SILO-031 | 350797-51-2 | 3-(indolin-1-yl)propyl benzoate hydrochloride |
| SILO-032 | 350797-52-3 | 3-(5-formylindolin-1-yl)propyl benzoate |
| SILO-033 | 79-24-3 | nitroethane |
| SILO-034 | 1404450-43-6 | (E)-3-(5-(2-nitroprop-1-en-1-yl)indolin-1-yl)propyl benzoate |
| SILO-035 | 350797-54-5 | 3-(5-(2-nitropropyl)indolin-1-yl)propyl benzoate |
| SILO-036 | 350797-55-6 | 3-(7-formyl-5-(2-nitropropyl)indolin-1-yl)propyl benzoate |
| SILO-037 | 350797-56-7 | 3-(7-cyano-5-(2-nitropropyl)indolin-1-yl)propyl benzoate |
| SILO-038 | 1338365-54-0 | 3-(5-(2-aminopropyl)-7-cyanoindolin-1-yl)propyl benzoate |
| SILO-039 | - | 2-(2-(2,2,2-trifluoroethoxy)phenoxy)acetyl chloride |
| SILO-040 | 1404450-39-0 | (R)-3-(7-cyano-5-(2-(2-(2-(2,2,2-trifluoroethoxy)phenoxy)acetamido)propyl)indolin-1-yl)propyl benzoate |
优化Route 4步骤 6 · 总收率 146.9 g
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| SILO-026 | 239463-72-0 | (R)-3-(5-(2-aminopropyl)-7-cyanoindolin-1-yl)propyl benzoate |
| SILO-027 | 885340-11-4 | (R)-3-(7-cyano-5-(2-((2-(2-(2,2,2-trifluoroethoxy)phenoxy)ethyl)amino)propyl)indolin-1-yl)propyl benzoate |
| SILO-030 | 942-95-0 | 3-chloropropyl benzoate |
| SILO-041 | 115661-82-0 | indoline-7-carbonitrile |
| SILO-042 | 1557330-03-6 | 3-(7-cyanoindolin-1-yl)propyl benzoate |
| SILO-043 | 1557330-14-9 | benzyl-D-alaninoyl chloride |
| SILO-044 | 1557330-06-9 | 3-(5-(benzyl-D-alanyl)-7-cyanoindolin-1-yl)propyl benzoate |
| SILO-045 | 1402161-30-1 | (R)-3-(5-(2-(benzylamino)propyl)-7-cyanoindolin-1-yl)propyl benzoate |
| SILO-046 | 160969-03-9 | 2-(2-(2,2,2-trifluoroethoxy)phenoxy)ethyl methanesulfonate |
工艺Route 5步骤 12 · 总收率 0.5 kg
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| SILO-029 | 496-15-1 | indoline |
| SILO-033 | 79-24-3 | nitroethane |
| SILO-046 | 160969-03-9 | 2-(2-(2,2,2-trifluoroethoxy)phenoxy)ethyl methanesulfonate |
| SILO-047 | 627-30-5 | 3-chloropropan-1-ol |
| SILO-048 | 26420-79-1 | ((3-chloropropoxy)methyl)benzene |
| SILO-049 | 459868-64-5 | 1-(3-(benzyloxy)propyl)indoline |
| SILO-050 | 459868-63-4 | 1-(3-(benzyloxy)propyl)indoline-5-carbaldehyde |
| SILO-051 | 1375180-28-1 | 1-(3-(benzyloxy)propyl)-7-bromoindoline-5-carbaldehyde |
| SILO-052 | 1375180-30-5 | 1-(3-(benzyloxy)propyl)-5-formylindoline-7-carbonitrile |
| SILO-053 | 1621480-46-3 | 1-(3-(benzyloxy)propyl)-5-(2-nitropropyl)indoline-7-carbonitrile |
| SILO-054 | 1096141-50-2 | 1-(3-(benzyloxy)propyl)-5-(2-oxopropyl)indoline-7-carbonitrile |
| SILO-055 | 196929-78-9 | (R)-2-methylpropane-2-sulfinamide |
| SILO-056 | 1621480-50-9 | (S)-N-(1-(1-(3-(benzyloxy)propyl)-7-cyanoindolin-5-yl)propan-2-yl)-2-methylpropane-2-sulfinamide |
| SILO-057 | 459868-73-6 (free) | (R)-5-(2-aminopropyl)-1-(3-(benzyloxy)propyl)indoline-7-carbonitrile 2-hydroxy-2-phenylacetate |
| SILO-058 | - | (R)-1-(3-(benzyloxy)propyl)-5-(2-((2-(2-(2,2,2-trifluoroethoxy)phenoxy)ethyl)amino)propyl)indoline-7-carbonitrile |
| SILO-059 | 175870-40-3 | (R)-1-(3-(benzyloxy)propyl)-5-(2-((2-(2-(2,2,2-trifluoroethoxy)phenoxy)ethyl)amino)propyl)indoline-7-carboxamide |
常见问题（FAQ）
赛洛多辛的适应症有哪些？
已批准的适应症包括：前列腺增生。
赛洛多辛的专利什么时候到期？
赛洛多辛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。
赛洛多辛有几条合成路线？
本站收录 5 条合成路线，最短路线 6 步、总收率 146.9 g。每条路线的中间体均带登记编号与 CAS 号。
赛洛多辛的关键中间体在哪里可以采购？
赛洛多辛的多条路线中间体已挂接 CAS 档案，其中 1 个 CAS 已有优贝德（Unibest）供应网络在售报价，可在本页路线表中直接查看并询价。
如何获取赛洛多辛中间体的报价？
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