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氟泽雷塞
Tier C · 观察 / 贸易Fulzerasib
劲方医药科技（上海）股份有限公司
原研
2024
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：KRAS G12C
商品名：Dupert、达伯特
适应症（已批准）：非小细胞肺癌
各地区研发/上市状态
美国
临床三期
2024-04-19
欧盟
临床二期
2023-04-25
中国
批准上市
2024-08-20
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 7 · 总收率 /
(I)1225102-1-a—(II)1225102-1-a—(III)1225102-1-a—(IV)1225102-1-a78495-63-3(V)1225102-1-a—(VI)1225102-1-a—(VII)1225102-1-a438631-77-7(VIII)1225102-1-a—(IX)1225102-1-a—(X)1225102-1-a74-88-4(XI)1225102-1-a,(XI)1225102-1-b—API · 氟泽雷塞
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)1225102-1-a | - | 6,7-Dichloro-1,2-dihydro-4-hydroxy-1-[4-methyl-2-(1-methylethyl)-3-pyridinyl]-2-oxo-1,8-naphthyridine-3-carbonitrile |
| (II)1225102-1-a | - | 6,7-Dichloro-4-hydroxy-1-(2-isopropyl-4-methyl-3-pyridyl)-1,8-naphthyridin-2-one |
| (III)1225102-1-a | - | 6,7-Dichloro-4-hydroxy-1-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-3-nitro-1,8-naphthyridin-2(1H)-one |
| (IV)1225102-1-a | 78495-63-3在售 | (2-Fluoro-6-methoxyphenyl)boronic acid |
| (V)1225102-1-a | - | 6-Chloro-7-(2-fluoro-6-methoxyphenyl)-4-hydroxy-1-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-3-nitro-1,8-naphthyridin-2(1H)-one |
| (VI)1225102-1-a | - | 4,6-Dichloro-7-(2-fluoro-6-methoxyphenyl)-1-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-3-nitro-1,8-naphthyridin-2(1H)-one |
| (VII)1225102-1-a | 438631-77-7 | (R)-Piperazine-1,3-dicarboxylic acid 1-tert-butyl 3-methyl diester |
| (VIII)1225102-1-a | - | 1-tert-Butyl 3-methyl (3R)-4-[6-chloro-7-(2-fluoro-6-methoxyphenyl)-1-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-3-nitro-2-oxo-1,2-dihydro-1,8-naphthyridin-4-yl]piperazine-1,3-dicarboxylate |
| (IX)1225102-1-a | - | tert-Butyl (4aR)-11-chloro-10-(2-fluoro-6-methoxyphenyl)-8-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-5,7-dioxo-1,2,4,4a,5,6,7,8-octahydro-3H-pyrazino[1',2':4,5]pyrazino[2,3-c][1,8]naphthyridine-3-carboxylate |
| (X)1225102-1-a | 74-88-4在售 | Iodomethane |
| (XI)1225102-1-a,(XI)1225102-1-b | - | tert-Butyl (4aR)-11-chloro-10-(2-fluoro-6-methoxyphenyl)-6-methyl-8-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-5,7-dioxo-1,2,4,4a,5,6,7,8-octahydro-3H-pyrazino[1',2':4,5]pyrazino[2,3-c][1,8]naphthyridine-3-carboxylate |
优化Route 2步骤 4 · 总收率 /
(XI)1225102-1-a,(XI)1225102-1-b—(XII)1225102-1-b—(XIII)1225102-1-b814-68-6(XIV)1225102-1-b—API · 氟泽雷塞
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (XI)1225102-1-a,(XI)1225102-1-b | - | tert-Butyl (4aR)-11-chloro-10-(2-fluoro-6-methoxyphenyl)-6-methyl-8-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-5,7-dioxo-1,2,4,4a,5,6,7,8-octahydro-3H-pyrazino[1',2':4,5]pyrazino[2,3-c][1,8]naphthyridine-3-carboxylate |
| (XII)1225102-1-b | - | (4aR)-11-Chloro-10-(2-fluoro-6-methoxyphenyl)-6-methyl-8-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-2,3,4,4a,6,8-hexahydro-1H-pyrazino[1',2':4,5]pyrazino[2,3-c][1,8]naphthyridine-5,7-dione |
| (XIII)1225102-1-b | 814-68-6在售 | 2-Propenoyl chloride |
| (XIV)1225102-1-b | - | (4aR)-11-Chloro-10-(2-fluoro-6-methoxyphenyl)-6-methyl-8-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-3-(prop-2-enoyl)-2,3,4,4a,6,8-hexahydro-1H-pyrazino[1',2':4,5]pyrazino[2,3-c][1,8]naphthyridine-5,7-dione |
优化Route 3步骤 5 · 总收率 /
(I)1225102-2-a38496-18-3(II)1225102-2-a1698293-93-4(III)1225102-2-a—(IV)1225102-2-a—(V)1225102-2-a—(VI)1225102-2-a—(VII)1225102-2-a127852-28-2(VIII)1225102-2-a2033-24-1(IX)1225102-2-a—(X)1225102-2-a1445-91-6(XIa)1225102-2-a—(XIb)1225102-2-a—(XII)1225102-2-a,(XII)1225102-2-b—(XIII)1225102-2-a—(XIV)1225102-2-a2216-51-5(XV)1225102-2-a—API · 氟泽雷塞
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)1225102-2-a | 38496-18-3 | 2,6-Dichloronicotinic acid |
| (II)1225102-2-a | 1698293-93-4在售 | 2-Isopropyl-4-methylpyridin-3-amine |
| (III)1225102-2-a | - | 6-Chloro-2-[(2-isopropyl-4-methyl-3-pyridyl)amino]pyridine-3-carboxylic acid |
| (IV)1225102-2-a | - | 5,6-Dichloro-2-[(2-isopropyl-4-methyl-3-pyridyl)amino]pyridine-3-carboxylic acid |
| (V)1225102-2-a | - | 5,6-Dichloro-2-[[4-methyl-2-(propan-2-yl)pyridin-3-yl]amino]pyridine-3-carbonyl chloride |
| (VI)1225102-2-a | - | 3-[(1R)-1-[3,5-Bis(trifluoromethyl)phenyl]ethoxy]-3-oxopropanoic acid |
| (VII)1225102-2-a | 127852-28-2 | (alphaR)-alpha-Methyl-3,5-bis(trifluoromethyl)benzenemethanol |
| (VIII)1225102-2-a | 2033-24-1 | 2,2-Dimethyl-1,3-dioxane-4,6-dione |
| (IX)1225102-2-a | - | 3-Oxo-3-[(1S)-1-phenylethoxy]propanoic acid |
| (X)1225102-2-a | 1445-91-6 | (1S)-Methyl phenyl carbinol |
| (XIa)1225102-2-a | - | (1S)-1-[3,5-Bis(trifluoromethyl)phenyl]ethyl 3-(5,6-dichloro-2-[[4-methyl-2-(propan-2-yl)pyridin-3-yl]amino]pyridin-3-yl)-3-oxopropanoate |
| (XIb)1225102-2-a | - | (1S)-1-Phenylethyl 3-(5,6-dichloro-2-[[4-methyl-2-(propan-2-yl)pyridin-3-yl]amino]pyridin-3-yl)-3-oxopropanoate |
| (XII)1225102-2-a,(XII)1225102-2-b | - | 6,7-Dichloro-4-hydroxy-1-(2-isopropyl-4-methyl-3-pyridyl)-1,8-naphthyridin-2-one |
| (XIII)1225102-2-a | - | 3-[(1R,2S,5R)-2-Isopropyl-5-methylcyclohexoxy]-3-oxo-propanoic acid |
| (XIV)1225102-2-a | 2216-51-5 | (-)-(1R-(1-alpha,2-beta,5-alpha))-5-Methyl-2-(1-methylethyl)cyclohexanol |
| (XV)1225102-2-a | - | (1R,2S,5R)-5-Methyl-2-(propan-2-yl)cyclohexyl 3-(5,6-dichloro-2-[[4-methyl-2-(propan-2-yl)pyridin-3-yl]amino]pyridin-3-yl)-3-oxopropanoate |
优化Route 4步骤 9 · 总收率 /
(aR)-(XVI)1225102-2-b—(XII)1225102-2-a,(XII)1225102-2-b—(XIX)1225102-2-b438631-77-7(XVII)1225102-2-b—(XVIII)1225102-2-b—(XX)1225102-2-b—(XXI)1225102-2-b—(XXII)1225102-2-b77-78-1(XXIII)1225102-2-b—(XXIV)1225102-2-b1256345-60-4(XXV)1225102-2-b—(XXVI)1225102-2-b—(XXVII)1225102-2-b814-68-6API · 氟泽雷塞
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (aR)-(XVI)1225102-2-b | - | (aR)-6,7-Dichloro-4-hydroxy-1-(2-isopropyl-4-methyl-3-pyridyl)-1,8-naphthyridin-2-one |
| (XII)1225102-2-a,(XII)1225102-2-b | - | 6,7-Dichloro-4-hydroxy-1-(2-isopropyl-4-methyl-3-pyridyl)-1,8-naphthyridin-2-one |
| (XIX)1225102-2-b | 438631-77-7 | (R)-Piperazine-1,3-dicarboxylic acid 1-tert-butyl 3-methyl diester |
| (XVII)1225102-2-b | - | (aR)-6,7-Dichloro-4-hydroxy-1-(2-isopropyl-4-methyl-3-pyridyl)-3-nitro-1,8-naphthyridin-2-one |
| (XVIII)1225102-2-b | - | (aR)-6,7-Dichloro-1-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-3-nitro-2-oxo-1,2-dihydro-1,8-naphthyridin-4-yl trifluoromethanesulfonate |
| (XX)1225102-2-b | - | (aR)-1-tert-Butyl 3-methyl (3R)-4-[6,7-dichloro-1-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-3-nitro-2-oxo-1,2-dihydro-1,8-naphthyridin-4-yl]piperazine-1,3-dicarboxylate |
| (XXI)1225102-2-b | - | (aR)-tert-Butyl (4aR)-10,11-dichloro-8-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-5,7-dioxo-1,2,4,4a,5,6,7,8-octahydro-3H-pyrazino[1',2':4,5]pyrazino[2,3-c][1,8]naphthyridine-3-carboxylate |
| (XXII)1225102-2-b | 77-78-1在售 | Dimethoxysulfone |
| (XXIII)1225102-2-b | - | (aR)-tert-Butyl (4aR)-10,11-dichloro-6-methyl-8-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-5,7-dioxo-1,2,4,4a,5,6,7,8-octahydro-3H-pyrazino[1',2':4,5]pyrazino[2,3-c][1,8]naphthyridine-3-carboxylate |
| (XXIV)1225102-2-b | 1256345-60-4在售 | (2-Fluoro-6-hydroxyphenyl)boronic acid |
| (XXV)1225102-2-b | - | (aR)-tert-Butyl (4aR)-11-chloro-10-(2-fluoro-6-hydroxyphenyl)-6-methyl-8-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-5,7-dioxo-1,2,4,4a,5,6,7,8-octahydro-3H-pyrazino[1',2':4,5]pyrazino[2,3-c][1,8]naphthyridine-3-carboxylate |
| (XXVI)1225102-2-b | - | (aR)-(4aR)-11-Chloro-10-(2-fluoro-6-hydroxyphenyl)-6-methyl-8-[4-methyl-2-(propan-2-yl)pyridin-3-yl]-2,3,4,4a,6,8-hexahydro-1H-pyrazino[1',2':4,5]pyrazino[2,3-c][1,8]naphthyridine-5,7-dione |
| (XXVII)1225102-2-b | 814-68-6在售 | 2-Propenoyl chloride |
常见问题（FAQ）
氟泽雷塞的适应症有哪些？
已批准的适应症包括：非小细胞肺癌。
氟泽雷塞的专利什么时候到期？
氟泽雷塞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。
氟泽雷塞有几条合成路线？
本站收录 4 条合成路线，最短路线 4 步、总收率 /。每条路线的中间体均带登记编号与 CAS 号。
氟泽雷塞的关键中间体在哪里可以采购？
氟泽雷塞的多条路线中间体已挂接 CAS 档案，其中 6 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。
如何获取氟泽雷塞中间体的报价？
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） · 2026-09-27