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可美替尼
Tier C · 观察 / 贸易Cobimetinib Fumarate · 2029 年到期全部品种 →
Exelixis Inc
原研
2015
首批上市
2029
到期年（公开口径）
$0.2B *
峰值销售
化学药
类型
靶点：MEK2、MEK1
商品名：Cotellic
适应症（已批准）：黑色素瘤
各地区研发/上市状态
美国
批准上市
2015-11-10
欧盟
批准上市
2015-02-27
中国
临床一期
2017-06-09
日本
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合成路线与中间体3 routes
原研路线 × 1优化路线（非专利）× 1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 10 · 总收率 /
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| COBI-001 | 18621-18-6 | azetidin-3-ol hydrochloride |
| COBI-002 | 128117-22-6 | benzyl 3-hydroxyazetidine-1-carboxylate |
| COBI-003 | 105258-93-3 | benzyl 3-oxoazetidine-1-carboxylate |
| COBI-004 | 75844-69-8 | tert-butyl piperidine-1-carboxylate |
| COBI-005 | 934664-27-4 | tert-butyl 2-(1-((benzyloxy)carbonyl)-3-hydroxyazetidin-3-yl)piperidine-1-carboxylate |
| COBI-006 | 39637-99-5 | (R)-3,3,3-trifluoro-2-methoxy-2-phenylpropanoyl chloride |
| COBI-007 | 934665-53-9 | (S)-tert-butyl 2-(1-((benzyloxy)carbonyl)-3-(((R)-3,3,3-trifluoro-2-methoxy-2-phenylpropanoyl)oxy)azetidin-3-yl)piperidine-1-carboxylate |
| COBI-008 | 934665-55-1 | (S)-tert-butyl 2-(1-((benzyloxy)carbonyl)-3-hydroxyazetidin-3-yl)piperidine-1-carboxylate |
| COBI-009 | 934666-39-4 | (S)-tert-butyl 2-(3-hydroxyazetidin-3-yl)piperidine-1-carboxylate |
| COBI-010 | 934664-19-4 | 3,4-difluoro-2-((2-fluoro-4-iodophenyl)amino)benzoyl fluoride |
| COBI-011 | 934663-52-2 | (S)-tert-butyl 2-(1-(3,4-difluoro-2-((2-fluoro-4-iodophenyl)amino)benzoyl)-3-hydroxyazetidin-3-yl)piperidine-1-carboxylate |
| COBI-012 | 61079-72-9 | 2,3,4-trifluorobenzoic acid |
| COBI-013 | 29632-74-4在售 | 2-fluoro-4-iodoaniline |
| COBI-014 | 391211-97-5 | 3,4-difluoro-2-((2-fluoro-4-iodophenyl)amino)benzoic acid |
| COBI-015 | 675-14-9 | 2,4,6-trifluoro-1,3,5-triazine |
优化Route 2步骤 6 · 总收率 20.66 g
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| COBI-012 | 61079-72-9 | 2,3,4-trifluorobenzoic acid |
| COBI-013 | 29632-74-4在售 | 2-fluoro-4-iodoaniline |
| COBI-016 | 106565-71-3 | (3S,5R,8aS)-3-phenylhexahydro-2H-oxazolo[3,2-a]pyridine-5-carbonitrile |
| COBI-017 | 398489-26-4 | tert-butyl 3-oxoazetidine-1-carboxylate |
| COBI-018 | 1597407-55-0 | tert-butyl 3-((3S,5R,8aS)-5-cyano-3-phenylhexahydro-2H-oxazolo[3,2-a]pyridin-5-yl)-3-hydroxyazetidine-1-carboxylate |
| COBI-019 | 1597407-56-1 | tert-butyl 3-hydroxy-3-((S)-1-((S)-2-hydroxy-1-phenylethyl)piperidin-2-yl)azetidine-1-carboxylate |
| COBI-020 | 1597407-57-2 (Freebase) | 3-((S)-1-((S)-2-hydroxy-1-phenylethyl)piperidin-2-yl)azetidin-3-ol |
| COBI-021 | 1597407-58-3 | (3-hydroxy-3-((S)-1-((S)-2-hydroxy-1-phenylethyl)piperidin-2-yl)azetidin-1-yl)(2,3,4-trifluorophenyl)methanone |
| COBI-022 | 1597407-59-4 (Freebase) | (S)-(3-hydroxy-3-(piperidin-2-yl)azetidin-1-yl)(2,3,4-trifluorophenyl)methanone hydrochloride |
工艺Route 3步骤 8 · 总收率 102.6 g
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| COBI-011 | 934663-52-2 | (S)-tert-butyl 2-(1-(3,4-difluoro-2-((2-fluoro-4-iodophenyl)amino)benzoyl)-3-hydroxyazetidin-3-yl)piperidine-1-carboxylate |
| COBI-017 | 398489-26-4 | tert-butyl 3-oxoazetidine-1-carboxylate |
| COBI-023 | 109-04-6 | 2-bromopyridine |
| COBI-024 | 1415560-24-5 | tert-butyl 3-hydroxy-3-(pyridin-2-yl)azetidine-1-carboxylate |
| COBI-025 | 1415564-55-4 | - |
| COBI-026 | 1415560-00-7 | 2,2,2-trifluoro-1-(3-hydroxy-3-(pyridin-2-yl)azetidin-1-yl)ethanone hydrochloride |
| COBI-027 | 1799970-85-6 | 2,2,2-trifluoro-1-(3-hydroxy-3-(piperidin-2-yl)azetidin-1-yl)ethanone hydrochloride |
| COBI-028 | 1415559-54-4 | tert-butyl 2-(3-hydroxy-1-(2,2,2-trifluoroacetyl)azetidin-3-yl)piperidine-1-carboxylate |
| COBI-029 | 934666-06-5 | tert-butyl 2-(3-hydroxyazetidin-3-yl)piperidine-1-carboxylate |
| COBI-030 | 833451-96-0 | 3,4-difluoro-2-((2-fluoro-4-iodophenyl)amino)benzoyl chloride |
常见问题（FAQ）
可美替尼的适应症有哪些？
已批准的适应症包括：黑色素瘤。
可美替尼的专利什么时候到期？
按公开口径，可美替尼的专利到期年为 2029 年。
可美替尼有几条合成路线？
本站收录 3 条合成路线，最短路线 6 步、总收率 20.66 g。每条路线的中间体均带登记编号与 CAS 号。
可美替尼的关键中间体在哪里可以采购？
可美替尼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。
如何获取可美替尼中间体的报价？
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