Norketotifen

Tier C · 观察 / 贸易

Norketotifen

Emergo Therapeutics Inc

原研

首批上市

到期年（公开口径）

无销量数据

峰值销售

化学药

类型

靶点：HRH1

适应症（已批准）：流感病毒感染、变应性结膜炎、过敏性鼻炎

各地区研发/上市状态

美国

临床二期

2019-04-01

欧盟

中国

日本

合成路线与中间体4 routes

原研路线 × 0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。

优化Route 1步骤 1 · 总收率 14.74 g (Norketotifen)

Ketotifen34580-13-7Norketotifen34580-20-6API · Norketotifen

编号	CAS 号	中间体名称
Ketotifen	34580-13-7	4-(1-methylpiperidin-4-ylidene)-4H-benzo[4,5]cyclohepta[1,2-b]thiophen-10(9H)-one
Norketotifen	34580-20-6	4-(piperidin-4-ylidene)-4H-benzo[4,5]cyclohepta[1,2-b]thiophen-10(9H)-one

优化Route 2步骤 7 · 总收率 /

(I)471701-1-a4506-53-0(II)471701-1-a,(II)471701-1-b34580-10-4(III)471701-1-a43076-89-7(IV)471701-1-a59743-84-9(V)471701-1-a,(V)471701-1-b63463-36-5(VI)471701-1-a5570-77-4(VII)471701-1-a59743-88-3(VIII)471701-1-a,(VIII)471701-1-b34580-13-7(IXa)471701-1-a34580-19-3(IXb)471701-1-a—API · Norketotifen

编号	CAS 号	中间体名称
(I)471701-1-a	4506-53-0	6-Thiatricyclo[8.4.0.0(3,7)]tetradeca-1(14),3(7),4,8,10,12-hexaen-2-one
(II)471701-1-a,(II)471701-1-b	34580-10-4	8,9-Dibromo-6-thiatricyclo[8.4.0.0(3,7)]tetradeca-1(10),3(7),4,11,13-pentaen-2-one
(III)471701-1-a	43076-89-7	9-Bromo-10-methoxy-9,10-dihydro-4H-benzo[4,5]cyclohepta[1,2-b]thiophen-4-one
(IV)471701-1-a	59743-84-9 在售	10-Methoxy-4H-benzo[4,5]cyclohepta[1,2-b]thiophen-4-one
(V)471701-1-a,(V)471701-1-b	63463-36-5	1-Methylpiperidn-4-ylmagnesium chloride
(VI)471701-1-a	5570-77-4	4-Chloro-1-methylpiperidine
(VII)471701-1-a	59743-88-3	10-Methoxy-4-(1-methylpiperidin-4-yl)-4H-benzo[4,5]cyclohepta[1,2-b]thiophene-4-ol
(VIII)471701-1-a,(VIII)471701-1-b	34580-13-7	4-(1-Methyl-4-piperidinylidene)-4,9-dihydro-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-one
(IXa)471701-1-a	34580-19-3	4-[8-Oxo-6-thiatricyclo[8.4.0.0(3,7)]tetradeca-1(14),3(7),4,10,12-pentaen-2-ylidene]piperidine-1-carboxylic acid ethyl ester
(IXb)471701-1-a	-	1-Chloroethyl 4-(10-oxo-9,10-dihydro-4H-benzo[4,5]cyclohepta[1,2-b]thiophen-4-ylidene)piperidine-1-carboxylate

优化Route 3步骤 6 · 总收率 /

(II)471701-1-a,(II)471701-1-b34580-10-4(V)471701-1-a,(V)471701-1-b63463-36-5(VIII)471701-1-a,(VIII)471701-1-b34580-13-7(X)471701-1-b1622-55-5(XI)471701-1-b34580-11-5(XII)471701-1-b59776-37-3(XIII)471701-1-b34580-12-6(XIV)471701-1-b110-89-4(XV)471701-1-b59743-85-0(XVI)471701-1-b59743-86-1(XVII)471701-1-b34580-09-1API · Norketotifen

编号	CAS 号	中间体名称
(II)471701-1-a,(II)471701-1-b	34580-10-4	8,9-Dibromo-6-thiatricyclo[8.4.0.0(3,7)]tetradeca-1(10),3(7),4,11,13-pentaen-2-one
(V)471701-1-a,(V)471701-1-b	63463-36-5	1-Methylpiperidn-4-ylmagnesium chloride
(VIII)471701-1-a,(VIII)471701-1-b	34580-13-7	4-(1-Methyl-4-piperidinylidene)-4,9-dihydro-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-one
(X)471701-1-b	1622-55-5 在售	6-thiatricyclo[8.4.0.0(3,7)]tetradeca-1(10),3(7),4,11,13-pentaen-2-one
(XI)471701-1-b	34580-11-5	8-bromo-6-thiatricyclo[8.4.0.0(3,7)]tetradeca-1(10),3(7),4,8,11,13-hexaen-2-one
(XII)471701-1-b	59776-37-3	8-bromo-2-(1-methylpiperidin-4-yl)-6-thiatricyclo[8.4.0.0(3,7)]tetradeca-1(10),3(7),4,8,11,13-hexaen-2-ol
(XIII)471701-1-b	34580-12-6	4-{8-bromo-6-thiatricyclo[8.4.0.0(3,7)]tetradeca-1(10),3(7),4,8,11,13-hexaen-2-ylidene}-1-methylpiperidine
(XIV)471701-1-b	110-89-4	Azacyclohexane
(XV)471701-1-b	59743-85-0	1-Methyl-4-[9-(piperidin-1-yl)-6-thiatricyclo[8.4.0.0(3,7)]tetradeca-1(14),3(7),4,8,10,12-hexaen-2-ylidene]piperidine
(XVI)471701-1-b	59743-86-1	1-methyl-4-[8-(piperidin-1-yl)-6-thiatricyclo[8.4.0.0(3,7)]tetradeca-1(10),3(7),4,8,11,13-hexaen-2-ylidene]piperidine
(XVII)471701-1-b	34580-09-1	2-(1-Methylpiperidin-4-ylidene)-6-thiatricyclo[8.4.0.0(3,7)]tetradeca-1(14),3(7),4,10,12-pentaen-9-one

优化Route 4步骤 2 · 总收率 /

(I)471701-2-a34580-13-7(IIa)471701-2-a108-24-7(IIb)471701-2-a1609-47-8(IIc)471701-2-a123-62-6(IId)471701-2-a93-97-0(IIe)471701-2-a31139-36-3(IIf)471701-2-a106-31-0(IIIa)471701-2-a117540-07-5(IIIb)471701-2-a34580-19-3(IIIc)471701-2-a2489527-25-3(IIId)471701-2-a2489527-27-5(IIIe)471701-2-a2489527-28-6(IIIf)471701-2-a2489527-26-4API · Norketotifen

编号	CAS 号	中间体名称
(I)471701-2-a	34580-13-7	4-(1-Methyl-4-piperidinylidene)-4,9-dihydro-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-one
(IIa)471701-2-a	108-24-7	Acetic acid acetic anhydride
(IIb)471701-2-a	1609-47-8	Dicarbonic acid diethyl diester
(IIc)471701-2-a	123-62-6 在售	Methylacetic anhydride
(IId)471701-2-a	93-97-0	Benzoic acid anhydride
(IIe)471701-2-a	31139-36-3	Dibenzyl dicarbonate
(IIf)471701-2-a	106-31-0	Butanoic acid 1-oxobutyl ester
(IIIa)471701-2-a	117540-07-5	4-(1-Acetylpiperidin-4-ylidene)-4,9-dihydro-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-one
(IIIb)471701-2-a	34580-19-3	4-[8-Oxo-6-thiatricyclo[8.4.0.0(3,7)]tetradeca-1(14),3(7),4,10,12-pentaen-2-ylidene]piperidine-1-carboxylic acid ethyl ester
(IIIc)471701-2-a	2489527-25-3	4-(1-Propanoylpiperidin-4-ylidene)-4,9-dihydro-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-one
(IIId)471701-2-a	2489527-27-5	4-(1-Benzoylpiperidin-4-ylidene)-4,9-dihydro-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-one
(IIIe)471701-2-a	2489527-28-6	Benzyl 4-(10-oxo-9,10-dihydro-4H-benzo[4,5]cyclohepta[1,2-b]thiophen-4-ylidene)piperidine-1-carboxylate
(IIIf)471701-2-a	2489527-26-4	4-(1-Butanoylpiperidin-4-ylidene)-4,9-dihydro-10H-benzo[4,5]cyclohepta[1,2-b]thiophen-10-one

常见问题（FAQ）

Norketotifen的适应症有哪些？

已批准的适应症包括：流感病毒感染、变应性结膜炎、过敏性鼻炎。

Norketotifen的专利什么时候到期？

Norketotifen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。

Norketotifen有几条合成路线？

本站收录 4 条合成路线，最短路线 1 步、总收率 14.74 g (Norketotifen)。每条路线的中间体均带登记编号与 CAS 号。

Norketotifen的关键中间体在哪里可以采购？

Norketotifen的多条路线中间体已挂接 CAS 档案，其中 3 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Norketotifen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） · 2026-10-08