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卡巴他赛
Tier C · 观察 / 贸易Cabazitaxel
赛诺菲
原研
2010
首批上市
-
到期年(公开口径)
$0.66B ▲
峰值销售
化学药
类型
靶点:Tubulin
商品名:Jevtana
适应症(已批准):前列腺癌
各地区研发/上市状态
美国
批准上市
2010-06-17
欧盟
批准上市
2011-03-17
中国
临床二期
2018-10-08
日本
批准上市
2014-07-04
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 3 · 总收率 350 mg
CABA-001859498-31-0CABA-0021354900-65-4CABA-0031638286-66-4API · 卡巴他赛
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| CABA-001 | 859498-31-0 | 5-((2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12b-acetoxy-12-(benzoyloxy)-11-hydroxy-4a,8,13,13-tetramethyl-5-oxo-4,6-bis(((2,2,2-trichloroethoxy)carbonyl)oxy)-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxet-9-yl) 3-(tert-butyl) (4S,5R)-2-(4-methoxyphenyl)-4-phenyloxazolidine-3,5-dicarboxylate |
| CABA-002 | 1354900-65-4 | 5-((2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12b-acetoxy-12-(benzoyloxy)-4,6,11-trihydroxy-4a,8,13,13-tetramethyl-5-oxo-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxet-9-yl) 3-(tert-butyl) (4S,5R)-2-(4-methoxyphenyl)-4-phenyloxazolidine-3,5-dicarboxylate |
| CABA-003 | 1638286-66-4 | 5-((2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12b-acetoxy-12-(benzoyloxy)-11-hydroxy-4a,8,13,13-tetramethyl-4,6-bis((methylthio)methoxy)-5-oxo-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxet-9-yl) 3-(tert-butyl) (4S,5R)-2-(4-methoxyphenyl)-4-phenyloxazolidine-3,5-dicarboxylate |
优化Route 2步骤 7 · 总收率 5.18 g
CABA-00432981-86-5CABA-00595603-44-4CABA-0063587-60-8CABA-0071396600-73-9CABA-0081396600-81-9CABA-0091396600-89-7CABA-010—CABA-011196404-55-4CABA-0121446010-46-3API · 卡巴他赛
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| CABA-004 | 32981-86-5 | (2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12b-acetoxy-4,6,9,11-tetrahydroxy-4a,8,13,13-tetramethyl-5-oxo-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxet-12-yl benzoate |
| CABA-005 | 95603-44-4 | (2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12b-acetoxy-9,11-dihydroxy-4a,8,13,13-tetramethyl-5-oxo-4,6-bis(((2,2,2-trichloroethoxy)carbonyl)oxy)-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxet-12-yl benzoate |
| CABA-006 | 3587-60-8在售 | ((chloromethoxy)methyl)benzene |
| CABA-007 | 1396600-73-9 | (2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12b-acetoxy-9-((benzyloxy)methoxy)-11-hydroxy-4a,8,13,13-tetramethyl-5-oxo-4,6-bis(((2,2,2-trichloroethoxy)carbonyl)oxy)-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxet-12-yl benzoate |
| CABA-008 | 1396600-81-9 | (2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12b-acetoxy-9-((benzyloxy)methoxy)-4,6,11-trihydroxy-4a,8,13,13-tetramethyl-5-oxo-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxet-12-yl benzoate |
| CABA-009 | 1396600-89-7 | (2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12b-acetoxy-9-((benzyloxy)methoxy)-11-hydroxy-4,6-dimethoxy-4a,8,13,13-tetramethyl-5-oxo-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxet-12-yl benzoate |
| CABA-010 | - | (2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12b-acetoxy-9,11-dihydroxy-4,6-dimethoxy-4a,8,13,13-tetramethyl-5-oxo-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxet-12-yl benzoate |
| CABA-011 | 196404-55-4 | (4S,5R)-3-(tert-butoxycarbonyl)-2-(4-methoxyphenyl)-4-phenyloxazolidine-5-carboxylic acid |
| CABA-012 | 1446010-46-3 | 5-((2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12b-acetoxy-12-(benzoyloxy)-4,11-dihydroxy-6-methoxy-4a,8,13,13-tetramethyl-5-oxo-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxet-9-yl) 3-(tert-butyl) (4S,5R)-2-(4-methoxyphenyl)-4-phenyloxazolidine-3,5-dicarboxylate |
优化Route 4步骤 4 · 总收率 34.5 g
CABA-00432981-86-5CABA-015207680-14-6CABA-0161444818-19-2CABA-0171444818-14-7API · 卡巴他赛
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| CABA-004 | 32981-86-5 | (2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12b-acetoxy-4,6,9,11-tetrahydroxy-4a,8,13,13-tetramethyl-5-oxo-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxet-12-yl benzoate |
| CABA-015 | 207680-14-6 | (2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12b-acetoxy-4,9,11-trihydroxy-4a,8,13,13-tetramethyl-5-oxo-6-((trimethylsilyl)oxy)-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxet-12-yl benzoate |
| CABA-016 | 1444818-19-2 | (2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12b-acetoxy-9,11-dihydroxy-4-methoxy-4a,8,13,13-tetramethyl-5-oxo-6-((trimethylsilyl)oxy)-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxet-12-yl benzoate |
| CABA-017 | 1444818-14-7 | (2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12b-acetoxy-6,9,11-trihydroxy-4-methoxy-4a,8,13,13-tetramethyl-5-oxo-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxet-12-yl benzoate |
优化Route 5步骤 3 · 总收率 3.93 g
CABA-001859498-31-0CABA-0021354900-65-4CABA-0181354900-66-5API · 卡巴他赛
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| CABA-001 | 859498-31-0 | 5-((2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12b-acetoxy-12-(benzoyloxy)-11-hydroxy-4a,8,13,13-tetramethyl-5-oxo-4,6-bis(((2,2,2-trichloroethoxy)carbonyl)oxy)-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxet-9-yl) 3-(tert-butyl) (4S,5R)-2-(4-methoxyphenyl)-4-phenyloxazolidine-3,5-dicarboxylate |
| CABA-002 | 1354900-65-4 | 5-((2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12b-acetoxy-12-(benzoyloxy)-4,6,11-trihydroxy-4a,8,13,13-tetramethyl-5-oxo-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxet-9-yl) 3-(tert-butyl) (4S,5R)-2-(4-methoxyphenyl)-4-phenyloxazolidine-3,5-dicarboxylate |
| CABA-018 | 1354900-66-5 | 5-((2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12b-acetoxy-12-(benzoyloxy)-11-hydroxy-4,6-dimethoxy-4a,8,13,13-tetramethyl-5-oxo-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxet-9-yl) 3-(tert-butyl) (4R,5R)-2-(4-methoxyphenyl)-4-phenyloxazolidine-3,5-dicarboxylate |
工艺Route 3步骤 2 · 总收率 0.77 kg
CABA-013162871-12-7CABA-0141380584-07-5API · 卡巴他赛
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| CABA-013 | 162871-12-7 | (2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12b-acetoxy-9-(((2R,3S)-3-((tert-butoxycarbonyl)amino)-3-phenyl-2-((triethylsilyl)oxy)propanoyl)oxy)-4,6,11-trihydroxy-4a,8,13,13-tetramethyl-5-oxo-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxet-12-yl benzoate |
| CABA-014 | 1380584-07-5 | (2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12b-acetoxy-9-(((2R,3S)-3-((tert-butoxycarbonyl)amino)-3-phenyl-2-((triethylsilyl)oxy)propanoyl)oxy)-11-hydroxy-4,6-dimethoxy-4a,8,13,13-tetramethyl-5-oxo-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxet-12-yl benzoate |
常见问题(FAQ)
卡巴他赛的适应症有哪些?
已批准的适应症包括:前列腺癌。
卡巴他赛的专利什么时候到期?
卡巴他赛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。
卡巴他赛有几条合成路线?
本站收录 5 条合成路线,最短路线 2 步、总收率 0.77 kg。每条路线的中间体均带登记编号与 CAS 号。
卡巴他赛的关键中间体在哪里可以采购?
卡巴他赛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。
如何获取卡巴他赛中间体的报价?
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