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甲苯磺酸依仑司群
Tier C · 观察 / 贸易Imlunestrant Tosylate
礼来制药
原研
2025
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：ERs
商品名：择叙、Inluriyo
适应症（已批准）：乳腺癌、转移性乳腺癌
各地区研发/上市状态
美国
批准上市
2025-09-25
欧盟
批准上市
2026-01-09
中国
批准上市
2026-06-17
日本
批准上市
2025-12-22
合成路线与中间体5 routes
原研路线 × 0优化路线（非专利）× 5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 7 · 总收率 /
(I)1078735-1-a1208452-88-3(II)1078735-1-a403-43-0(III)1078735-1-a2408771-98-0(IV)1078735-1-a2408771-99-1(V)1078735-1-a2303565-96-8(VI)1078735-1-a2408772-00-7(VII)1078735-1-a503309-11-3(VIII)1078735-1-a2408771-96-8(IX)1078735-1-a—(X)1078735-1-a2408771-97-9(XI)1078735-1-a1642298-59-6(XII)1078735-1-a23147-58-2(XIII)1078735-1-a1443983-86-5API · 甲苯磺酸依仑司群
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)1078735-1-a | 1208452-88-3 | 4-Bromo-3-chloro-7-methoxyquinoline |
| (II)1078735-1-a | 403-43-0在售 | 4-Fluoranylbenzoyl chloride |
| (III)1078735-1-a | 2408771-98-0 | (3-Chloro-7-methoxyquinolin-4-yl)(4-fluorophenyl)methanone |
| (IV)1078735-1-a | 2408771-99-1 | (3-Chloro-7-hydroxyquinolin-4-yl)(4-fluorophenyl)methanone |
| (V)1078735-1-a | 2303565-96-8 | 2-[3-(Fluoromethyl)azetidin-1-yl]ethan-1-ol hydrogen chloride |
| (VI)1078735-1-a | 2408772-00-7 | (3-Chloro-7-hydroxyquinolin-4-yl)(4-[2-[3-(fluoromethyl)azetidin-1-yl]ethoxy]phenyl)methanone |
| (VII)1078735-1-a | 503309-11-3 | [2-Fluoro-4-(trifluoromethyl)phenyl]boronic acid |
| (VIII)1078735-1-a | 2408771-96-8 | (4-[2-[3-(Fluoromethyl)azetidin-1-yl]ethoxy]phenyl)[3-[2-fluoro-4-(trifluoromethyl)phenyl]-7-hydroxyquinolin-4-yl]methanone |
| (IX)1078735-1-a | - | 4-[(4-[2-[3-(Fluoromethyl)azetidin-1-yl]ethoxy]phenyl)(hydroxy)methyl]-3-[2-fluoro-4-(trifluoromethyl)phenyl]quinolin-7-ol |
| (X)1078735-1-a | 2408771-97-9 | 5-(4-[2-[3-(Fluoromethyl)azetidin-1-yl]ethoxy]phenyl)-8-(trifluoromethyl)-5H-[1]benzopyrano[4,3-c]quinolin-2-ol |
| (XI)1078735-1-a | 1642298-59-6 | 3-(Fluoromethyl)azetidine hydrogen chloride |
| (XII)1078735-1-a | 23147-58-2 | 1,4-Dioxane-2,5-diol |
| (XIII)1078735-1-a | 1443983-86-5 | 2-[3-(Fluoromethyl)azetidin-1-yl]ethan-1-ol |
优化Route 2步骤 8 · 总收率 /
(I)1078735-2-a82121-05-9(II)1078735-2-a1203579-66-1(III)1078735-2-a1208452-88-3(IV)1078735-2-a459-57-4(V)1078735-2-a2408771-98-0(VI)1078735-2-a403-43-0(VII)1078735-2-a2408771-99-1(VIII)1078735-2-a621-63-6(IX)1078735-2-a—(X)1078735-2-a503309-11-3(XI)1078735-2-a—(XII)1078735-2-a2408772-01-8(XIII)1078735-2-a—(XIV)1078735-2-a,(XIV)1078735-2-b—API · 甲苯磺酸依仑司群
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)1078735-2-a | 82121-05-9 | 4-Hydroxy-7-methoxyquinoline |
| (II)1078735-2-a | 1203579-66-1 | 3-Chloro-4-hydroxy-7-methoxyquinoline |
| (III)1078735-2-a | 1208452-88-3 | 4-Bromo-3-chloro-7-methoxyquinoline |
| (IV)1078735-2-a | 459-57-4 | (4-Fluorophenyl)methanone |
| (V)1078735-2-a | 2408771-98-0 | (3-Chloro-7-methoxyquinolin-4-yl)(4-fluorophenyl)methanone |
| (VI)1078735-2-a | 403-43-0在售 | 4-Fluoranylbenzoyl chloride |
| (VII)1078735-2-a | 2408771-99-1 | (3-Chloro-7-hydroxyquinolin-4-yl)(4-fluorophenyl)methanone |
| (VIII)1078735-2-a | 621-63-6 | 1,1-Diethoxy-2-hydroxyethane |
| (IX)1078735-2-a | - | (3-Chloro-7-hydroxyquinolin-4-yl)[4-(2,2-diethoxyethoxy)phenyl]methanone |
| (X)1078735-2-a | 503309-11-3 | [2-Fluoro-4-(trifluoromethyl)phenyl]boronic acid |
| (XI)1078735-2-a | - | [4-(2,2-Diethoxyethoxy)phenyl][3-[2-fluoro-4-(trifluoromethyl)phenyl]-7-hydroxyquinolin-4-yl]methanone |
| (XII)1078735-2-a | 2408772-01-8 | (4-Fluorophenyl)[3-[2-fluoro-4-(trifluoromethyl)phenyl]-7-hydroxyquinolin-4-yl]methanone |
| (XIII)1078735-2-a | - | 4-[(R)-[4-(2,2-Diethoxyethoxy)phenyl](hydroxy)methyl]-3-[2-fluoro-4-(trifluoromethyl)phenyl]quinolin-7-ol |
| (XIV)1078735-2-a,(XIV)1078735-2-b | - | (5R)-5-[4-(2,2-Diethoxyethoxy)phenyl]-8-(trifluoromethyl)-5H-[1]benzopyrano[4,3-c]quinolin-2-ol |
优化Route 3步骤 2 · 总收率 /
(XIV)1078735-2-a,(XIV)1078735-2-b—(XV)1078735-2-b—(XVI)1078735-2-b—(XVII)1078735-2-b—API · 甲苯磺酸依仑司群
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (XIV)1078735-2-a,(XIV)1078735-2-b | - | (5R)-5-[4-(2,2-Diethoxyethoxy)phenyl]-8-(trifluoromethyl)-5H-[1]benzopyrano[4,3-c]quinolin-2-ol |
| (XV)1078735-2-b | - | 2-[4-[(5R)-2-Hydroxy-8-(trifluoromethyl)-5H-[1]benzopyrano[4,3-c]quinolin-5-yl]phenoxy]ethane-1,1-diol |
| (XVI)1078735-2-b | - | 3-(Fluoromethyl)azetidine tosylate |
| (XVII)1078735-2-b | - | [4-[(5R)-2-Hydroxy-8-(trifluoromethyl)-5H-[1]benzopyrano[4,3-c]quinolin-5-yl]phenoxy]acetaldehyde |
优化Route 4步骤 6 · 总收率 /
(I)1078735-3-a1208452-88-3(II)1078735-3-a1071809-52-3(III)1078735-3-a—(IV)1078735-3-a—(V)1078735-3-a503309-11-3(VI)1078735-3-a—(VII)1078735-3-a1443983-86-5(VIII)1078735-3-a—(IX)1078735-3-a—(X)1078735-3-a—API · 甲苯磺酸依仑司群
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)1078735-3-a | 1208452-88-3 | 4-Bromo-3-chloro-7-methoxyquinoline |
| (II)1078735-3-a | 1071809-52-3 | 4-Fluoro-2,3,5,6-tetradeutero-benzoyl chloride |
| (III)1078735-3-a | - | (3-Chloro-7-methoxyquinolin-4-yl)[4-fluoro-2,3,5,6-tetradeutero-phenyl]methanone |
| (IV)1078735-3-a | - | (3-Chloro-7-hydroxyquinolin-4-yl)[4-fluoro-2,3,5,6-tetradeutero-phenyl]methanone |
| (V)1078735-3-a | 503309-11-3 | [2-Fluoro-4-(trifluoromethyl)phenyl]boronic acid |
| (VI)1078735-3-a | - | [4-Fluoro-2,3,5,6-tetradeutero-phenyl][3-[2-fluoro-4-(trifluoromethyl)phenyl]-7-hydroxyquinolin-4-yl]methanone |
| (VII)1078735-3-a | 1443983-86-5 | 2-[3-(Fluoromethyl)azetidin-1-yl]ethan-1-ol |
| (VIII)1078735-3-a | - | [4-[2-[3-(Fluoromethyl)azetidin-1-yl]ethoxy]-2,3,5,6-tetradeutero-phenyl][3-[2-fluoro-4-(trifluoromethyl)phenyl]-7-hydroxyquinolin-4-yl]methanone |
| (IX)1078735-3-a | - | 4-[[4-[2-[3-(Fluoromethyl)azetidin-1-yl]ethoxy]-2,3,5,6-tetradeutero-phenyl](hydroxy)methyl]-3-[2-fluoro-4-(trifluoromethyl)phenyl]quinolin-7-ol |
| (X)1078735-3-a | - | (±)-5-[4-[2-[3-(Fluoromethyl)azetidin-1-yl]ethoxy]-2,3,5,6-tetradeutero-phenyl]-8-(trifluoromethyl)-5H-[1]benzopyrano[4,3-c]quinolin-2-ol |
优化Route 5步骤 2 · 总收率 /
(I)1078735-4-a28027-17-0(II)1078735-4-a1431364-31-6(III)1078735-4-a503309-11-3(IV)1078735-4-a—API · 甲苯磺酸依仑司群
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)1078735-4-a | 28027-17-0 | 4-Hydroxy-7-methoxyquinoline-3-carboxylic acid |
| (II)1078735-4-a | 1431364-31-6 | 3-Iodo-7-methoxyquinolin-4-ol |
| (III)1078735-4-a | 503309-11-3 | [2-Fluoro-4-(trifluoromethyl)phenyl]boronic acid |
| (IV)1078735-4-a | - | 3-[2-Fluoro-4-(trifluoromethyl)phenyl]-7-methoxyquinolin-4-ol |
常见问题（FAQ）
甲苯磺酸依仑司群的适应症有哪些？
已批准的适应症包括：乳腺癌、转移性乳腺癌。
甲苯磺酸依仑司群的专利什么时候到期？
甲苯磺酸依仑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。
甲苯磺酸依仑司群有几条合成路线？
本站收录 5 条合成路线，最短路线 2 步、总收率 /。每条路线的中间体均带登记编号与 CAS 号。
甲苯磺酸依仑司群的关键中间体在哪里可以采购？
甲苯磺酸依仑司群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。
如何获取甲苯磺酸依仑司群中间体的报价？
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