氢溴酸依他佐辛

Tier C · 观察 / 贸易

Eptazocine hydrobromide

日医工株式会社

原研

首批上市

到期年（公开口径）

无销量数据

峰值销售

小分子

类型

靶点：MOR1、KOR1

商品名：Sedapain

适应症（已批准）：癌症疼痛、术后疼痛

各地区研发/上市状态

美国

欧盟

中国

批准上市

2006-05-25

日本

批准上市

1987-01-12

合成路线与中间体8 routes

原研路线 × 0优化路线（非专利）× 8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 5 · 总收率 /

M1—M2—M3—M4—M5—API · 氢溴酸依他佐辛

编号	CAS 号	中间体名称
-	-	(1R,9S)-1-methyl-11-azatricyclo[7.4.1.0(2,7)]tetradeca-2(7),3,5-trien-4-ol
-	-	ethyl (1R,9S)-4-hydroxy-1-methyl-11-azatricyclo[7.4.1.0(2,7)]tetradeca-2(7),3,5-triene-11-carboxylate
-	-	(1R,9R)-4-(benzyloxy)-1,11-dimethyl-11-azatricyclo[7.4.1.0(2,7)]tetradeca-2(7),3,5-trien-8-one
-	-	(1R,9S)-4-methoxy-1,11-dimethyl-11-azatricyclo[7.4.1.0(2,7)]tetradeca-2,4,6-triene
-	-	(6S,8R)-6-(bromomethyl)-8-methyl-8-[2-(methylamino)ethyl]-5,6,7,8-tetrahydronaphthalen-2-ol

优化Route 2步骤 3 · 总收率 /

M1—M2—M3—API · 氢溴酸依他佐辛

编号	CAS 号	中间体名称
-	-	(4R)-6-methoxy-4-methyl-4-[2-(methylamino)ethyl]-1,2,3,4-tetrahydronaphthalen-1-one
-	-	(1R,9R)-4-methoxy-1,11-dimethyl-11-azatricyclo[7.4.1.0(2,7)]tetradeca-2(7),3,5-trien-8-one
-	-	(1R,9R)-4-methoxy-1,11-dimethyl-11-azatricyclo[7.4.1.0(2,7)]tetradeca-2(7),3,5-trien-8-ol

优化Route 3步骤 1 · 总收率 /

M174958-17-1API · 氢溴酸依他佐辛

编号	CAS 号	中间体名称
-	74958-17-1	(1S,6S)-10-Methoxy-1,4-dimethyl-2,3,4,5,6,7-hexahydro-1H-1,6-methano-4-benzazonine

优化Route 4步骤 7 · 总收率 /

M11224714-08-2M23756-30-7M31430074-21-7M41430074-22-8M51430074-33-1M650-00-0M7—M8—M9—M10—API · 氢溴酸依他佐辛

编号	CAS 号	中间体名称
-	1224714-08-2	(4R)-4-Benzyl-3-[3-(4-methoxyphenyl)propanoyl]-1,3-oxazolidin-2-one
-	3756-30-7	Methylallyl iodide
-	1430074-21-7	(2R)-2-[(4-Methoxyphenyl)methyl]-4-methylpent-4-en-1-ol
-	1430074-22-8	1-[(2R)-2-(Azidomethyl)-4-methylpent-4-en-1-yl]-4-methoxybenzene
-	1430074-33-1	N-[(2R)-2-[(4-Methoxyphenyl)methyl]-4-methylpent-4-en-1-yl]-4-methylbenzene-1-sulfonamide
-	50-00-0 在售	Formalin
-	-	(1S,6R)-10-Methoxy-1-methyl-4-(4-methylbenzene-1-sulfonyl)-2,3,4,5,6,7-hexahydro-1H-1,6-methano-4-benzazonine
-	-	(1S,6R)-10-Methoxy-1-methyl-2,3,4,5,6,7-hexahydro-1H-1,6-methano-4-benzazonine
-	-	(1S,6R)-1,4-Dimethyl-2,3,4,5,6,7-hexahydro-1H-1,6-methano-4-benzazonin-10-ol
-	-	(1S,6R)-10-Methoxy-1,4-dimethyl-2,3,4,5,6,7-hexahydro-1H-1,6-methano-4-benzazonine

优化Route 5步骤 8 · 总收率 378g(Eptazocine-030)

M14746-97-8M25470-11-1M3180918-12-1M42087469-16-5M52087469-17-6M6172090-55-0M774-88-4M8879399-10-7M9824-94-2M102087469-19-8M1182160-88-1M1282160-89-2API · 氢溴酸依他佐辛

编号	CAS 号	中间体名称
-	4746-97-8	1,4-Dioxaspiro[4.5]decan-8-one
-	5470-11-1 在售	Hydroxylamine hydrochloride
-	180918-12-1	N-{1,4-dioxaspiro[4.5]decan-8-ylidene}hydroxylamine
-	2087469-16-5	N-[(Methanesulfonyl)oxy]-1,4-dioxaspiro[4.5]decan-8-imine
-	2087469-17-6	10-[(4-Methoxyphenyl)methyl]-8-methyl-1,4-dioxa-8-azaspiro[4.6]undecan-9-one
-	172090-55-0	1,4-Dioxa-8-azaspiro[4.6]undecan-9-one
-	74-88-4 在售	Iodomethane
-	879399-10-7	8-Methyl-1,4-dioxa-8-azaspiro[4.6]undecan-9-one
-	824-94-2	4-Methoxybenzyl chloride
-	2087469-19-8	4-Nitrobenzoic acid 10-[(4-methoxyphenyl)methyl]-8-methyl-1,4-dioxa-8-azaspiro[4.6]undecane
-	82160-88-1	6-[(4-Methoxyphenyl)methyl]-1-methylazepan-4-one
-	82160-89-2	6-[(4-Methoxyphenyl)methyl]-1,4-dimethylazepan-4-ol

优化Route 6步骤 4 · 总收率 8.2g(Eptazocine)

M12087469-20-1M22087469-21-2M354782-45-5M4—M582160-89-2API · 氢溴酸依他佐辛

编号	CAS 号	中间体名称
-	2087469-20-1	3-[(4-Methoxyphenyl)methyl]-1,5-dimethyl-2,3,6,7-tetrahydro-1H-azepine
-	2087469-21-2	3-[(4-Methoxyphenyl)methyl]-1,5-dimethyl-2,3,4,7-tetrahydro-1H-azepine
-	54782-45-5	10-Methoxy-1,4-dimethyl-2,3,4,5,6,7-hexahydro-1H-1,6-methano-4-benzazonine
-	-	(1S,6R)-10-Methoxy-1,4-dimethyl-2,3,4,5,6,7-hexahydro-1H-1,6-methano-4-benzazonine
-	82160-89-2	6-[(4-Methoxyphenyl)methyl]-1,4-dimethylazepan-4-ol

优化Route 7步骤 6 · 总收率 /

M1107623-21-2M2—M32222923-20-6M4593-51-1M5—M62222922-73-6M7713482-37-2M854782-51-3M950-00-0API · 氢溴酸依他佐辛

编号	CAS 号	中间体名称
-	107623-21-2	3-Benzyloxyiodobenzene
-	-	6-Iodo-3-methylhex-2(Z)-en-1-ol
-	2222923-20-6	[7-(Benzyloxy)-1-methyl-1,2,3,4-tetrahydronaphthalen-1-yl]acetaldehyde
-	593-51-1	Methanamine hydrochloride
-	-	1,4-Dimethyl-2,3,4,5,6,7-hexahydro-1H-1,6-methano-4-benzazonin-10-ol hydrogen bromide
-	2222922-73-6	2-[7-(Benzyloxy)-1-methyl-1,2,3,4-tetrahydronaphthalen-1-yl]-N-methylethan-1-amine
-	713482-37-2	10-(Benzyloxy)-1,4-dimethyl-1,2,3,4,5,6-hexahydro-7H-1,6-methano-4-benzazonin-7-one
-	54782-51-3	1,4-Dimethyl-2,3,4,5,6,7-hexahydro-1H-1,6-methano-4-benzazonin-10-ol
-	50-00-0 在售	Formaldehyde

优化Route 8步骤 6 · 总收率 106g(Eptazocine-046)

M11204-23-5M2105-36-2M332859-75-9M42671129-02-3M5122818-69-3M62671129-03-4M72671129-04-5M874-89-5M92671129-05-6API · 氢溴酸依他佐辛

编号	CAS 号	中间体名称
-	1204-23-5	7-Methoxy-1-methyl-3,4-dihydronaphthalen-2-one
-	105-36-2 在售	2-Bromoacetic acid ethyl ester
-	32859-75-9	Ethyl (7-methoxy-1-methyl-2-oxo-1,2,3,4-tetrahydronaphthalen-1-yl)acetate
-	2671129-02-3	Ethyl (2-hydroxy-7-methoxy-1-methyl-1,2,3,4-tetrahydronaphthalen-1-yl)acetate
-	122818-69-3	2-(7-Methoxy-1-methyl-1,2,3,4-tetrahydronaphthalen-1-yl)-N-methylethan-1-amine
-	2671129-03-4	Ethyl (7-methoxy-1-methyl-1,4-dihydronaphthalen-1-yl)acetate
-	2671129-04-5	Ethyl (7-methoxy-1-methyl-1,2,3,4-tetrahydronaphthalen-1-yl)acetate
-	74-89-5	Methylamine
-	2671129-05-6	2-(7-Methoxy-1-methyl-1,2,3,4-tetrahydronaphthalen-1-yl)-N-methylacetamide

常见问题（FAQ）

氢溴酸依他佐辛的适应症有哪些？

已批准的适应症包括：癌症疼痛、术后疼痛。

氢溴酸依他佐辛的专利什么时候到期？

氢溴酸依他佐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。

氢溴酸依他佐辛有几条合成路线？

本站收录 8 条合成路线，最短路线 1 步、总收率 /。每条路线的中间体均带登记编号与 CAS 号。

氢溴酸依他佐辛的关键中间体在哪里可以采购？

氢溴酸依他佐辛的多条路线中间体已挂接 CAS 档案，其中 4 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。

如何获取氢溴酸依他佐辛中间体的报价？

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） · 2026-10-21