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宗艾替尼
Tier C · 观察 / 贸易Zongertinib
Boehringer Ingelheim International Gmbh
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：HER2
商品名：HERNEXEOS、圣赫途
适应症（已批准）：非小细胞肺癌
各地区研发/上市状态
美国
批准上市
2025-08-08
欧盟
临床三期
2024-02-09
中国
批准上市
2025-08-26
日本
批准上市
2025-09-19
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)1157260-1-a455-88-9(II)1157260-1-a,(II)1157260-1-b—(III)1157260-1-a—(IV)1157260-1-a—(Va)1157260-1-a—(Vb)1157260-1-a—(VI)1157260-1-a—(VII)1157260-1-a—(VIII)1157260-1-a73874-95-0(IX)1157260-1-a—(X)1157260-1-a—(XI)1157260-1-a814-68-6API · 宗艾替尼
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)1157260-1-a | 455-88-9 | 1-Fluoro-2-methyl-4-nitrobenzene |
| (II)1157260-1-a,(II)1157260-1-b | - | 1-Methyl-1H-1,3-benzimidazol-5-ol |
| (III)1157260-1-a | - | 1-Methyl-5-(2-methyl-4-nitrophenoxy)-1H-1,3-benzimidazole |
| (IV)1157260-1-a | - | 3-Methyl-4-((1-methyl-1H-benzimidazol-5-yl)oxy)benzenamine |
| (Va)1157260-1-a | - | 4-Chloro-6-(methylthio)pyrimido[5,4-d]pyrimidine |
| (Vb)1157260-1-a | - | 8-Chloro-2-(methylsulfanyl)pyrimido[5,4-d]pyrimidine hydrogen chloride |
| (VI)1157260-1-a | - | N-[3-Methyl-4-[(1-methyl-1H-1,3-benzimidazol-5-yl)oxy]phenyl]-6-(methylsulfanyl)pyrimido[5,4-d]pyrimidin-4-amine |
| (VII)1157260-1-a | - | 6-(Methanesulfinyl)-N-[3-methyl-4-[(1-methyl-1H-1,3-benzimidazol-5-yl)oxy]phenyl]pyrimido[5,4-d]pyrimidin-4-amine |
| (VIII)1157260-1-a | 73874-95-0 | 1,1-Dimethylethyl piperidin-4-ylcarbamate |
| (IX)1157260-1-a | - | tert-Butyl [1-(8-[3-methyl-4-[(1-methyl-1H-1,3-benzimidazol-5-yl)oxy]anilino]pyrimido[5,4-d]pyrimidin-2-yl)piperidin-4-yl]carbamate |
| (X)1157260-1-a | - | 6-(4-Aminopiperidin-1-yl)-N-[3-methyl-4-[(1-methyl-1H-1,3-benzimidazol-5-yl)oxy]phenyl]pyrimido[5,4-d]pyrimidin-4-amine |
| (XI)1157260-1-a | 814-68-6在售 | 2-Propenoyl chloride |
优化Route 2步骤 4 · 总收率 /
(II)1157260-1-a,(II)1157260-1-b—(XII)1157260-1-b96-96-8(XIII)1157260-1-b74-88-4(XIV)1157260-1-b—(XV)1157260-1-b—(XVI)1157260-1-b3473-63-0(XVII)1157260-1-b—API · 宗艾替尼
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (II)1157260-1-a,(II)1157260-1-b | - | 1-Methyl-1H-1,3-benzimidazol-5-ol |
| (XII)1157260-1-b | 96-96-8 | 2-Nitro-p-anisidine |
| (XIII)1157260-1-b | 74-88-4在售 | Iodomethane |
| (XIV)1157260-1-b | - | 4-Methoxy-N-methyl-2-nitroaniline |
| (XV)1157260-1-b | - | 4-Methoxy-N1-methylbenzene-1,2-diamine |
| (XVI)1157260-1-b | 3473-63-0 | Aminomethylideneazanium acetate |
| (XVII)1157260-1-b | - | 5-Methoxy-1-methyl-1H-1,3-benzimidazole |
优化Route 3步骤 7 · 总收率 /
(I)1157260-2-a98550-19-7(II)1157260-2-a—(III)1157260-2-a,(III)1157260-2-b—(IVa)1157260-2-a—(IVb)1157260-2-a—(V)1157260-2-a—(VI)1157260-2-a73874-95-0(VII)1157260-2-a—(VIII)1157260-2-a—(IX)1157260-2-a625-36-5(X)1157260-2-a—API · 宗艾替尼
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)1157260-2-a | 98550-19-7 | 6-(Methylsulfanyl)-[1,3]diazino[5,4-d]pyrimidin-4-ol |
| (II)1157260-2-a | - | 4-Chloro-6-(methylthio)pyrimido[5,4-d]pyrimidine |
| (III)1157260-2-a,(III)1157260-2-b | - | 3-Methyl-4-((1-methyl-1H-benzimidazol-5-yl)oxy)benzenamine |
| (IVa)1157260-2-a | - | N-[3-Methyl-4-[(1-methyl-1H-1,3-benzimidazol-5-yl)oxy]phenyl]-6-(methylsulfanyl)pyrimido[5,4-d]pyrimidin-4-amine |
| (IVb)1157260-2-a | - | N-[3-Methyl-4-[(1-methyl-1H-1,3-benzimidazol-5-yl)oxy]phenyl]-6-(methylsulfanyl)pyrimido[5,4-d]pyrimidin-4-amine hydrogen chloride |
| (V)1157260-2-a | - | 6-(Methanesulfonyl)-N-[3-methyl-4-[(1-methyl-1H-1,3-benzimidazol-5-yl)oxy]phenyl]pyrimido[5,4-d]pyrimidin-4-amine |
| (VI)1157260-2-a | 73874-95-0 | 1,1-Dimethylethyl piperidin-4-ylcarbamate |
| (VII)1157260-2-a | - | tert-Butyl [1-(8-[3-methyl-4-[(1-methyl-1H-1,3-benzimidazol-5-yl)oxy]anilino]pyrimido[5,4-d]pyrimidin-2-yl)piperidin-4-yl]carbamate |
| (VIII)1157260-2-a | - | 6-(4-Aminopiperidin-1-yl)-N-[3-methyl-4-[(1-methyl-1H-1,3-benzimidazol-5-yl)oxy]phenyl]pyrimido[5,4-d]pyrimidin-4-amine hydrogen chloride (1/3) |
| (IX)1157260-2-a | 625-36-5在售 | (Chloromethyl)acetyl chloride |
| (X)1157260-2-a | - | 3-Chloro-N-[1-(8-[3-methyl-4-[(1-methyl-1H-1,3-benzimidazol-5-yl)oxy]anilino]pyrimido[5,4-d]pyrimidin-2-yl)piperidin-4-yl]propanamide |
优化Route 4步骤 5 · 总收率 /
(III)1157260-2-a,(III)1157260-2-b—(XI)1157260-2-b455-88-9(XII)1157260-2-b610-81-1(XIII)1157260-2-b—(XIV)1157260-2-b77-78-1(XV)1157260-2-b—(XVI)1157260-2-b—(XVII)1157260-2-b64-18-6(XVIII)1157260-2-b—API · 宗艾替尼
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (III)1157260-2-a,(III)1157260-2-b | - | 3-Methyl-4-((1-methyl-1H-benzimidazol-5-yl)oxy)benzenamine |
| (XI)1157260-2-b | 455-88-9 | 1-Fluoro-2-methyl-4-nitrobenzene |
| (XII)1157260-2-b | 610-81-1 | 4-Amino-3-nitrophenol |
| (XIII)1157260-2-b | - | 4-(2-Methyl-4-nitrophenoxy)-2-nitroaniline |
| (XIV)1157260-2-b | 77-78-1在售 | Dimethoxysulfone |
| (XV)1157260-2-b | - | N-Methyl-4-(2-methyl-4-nitrophenoxy)-2-nitroaniline |
| (XVI)1157260-2-b | - | 4-(4-Amino-2-methylphenoxy)-N1-methylbenzene-1,2-diamine |
| (XVII)1157260-2-b | 64-18-6 | Formic acid |
| (XVIII)1157260-2-b | - | N-[3-Methyl-4-[(1-methyl-1H-1,3-benzimidazol-5-yl)oxy]phenyl]formamide |
优化Route 5步骤 3 · 总收率 /
(I)1157260-3-a—(II)1157260-3-a—(III)1157260-3-a—(IV)1157260-3-a—API · 宗艾替尼
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)1157260-3-a | - | 6-(Methanesulfonyl)-N-[3-methyl-4-[(1-methyl-1H-1,3-benzimidazol-5-yl)oxy]phenyl]pyrimido[5,4-d]pyrimidin-4-amine |
| (II)1157260-3-a | - | 3-(Methylsulfanyl)-N-(piperidin-4-yl)propanamide |
| (III)1157260-3-a | - | N-[1-(8-[3-Methyl-4-[(1-methyl-1H-1,3-benzimidazol-5-yl)oxy]anilino]pyrimido[5,4-d]pyrimidin-2-yl)piperidin-4-yl]-3-(methylsulfanyl)propanamide |
| (IV)1157260-3-a | - | 3-(Methanesulfonyl)-N-[1-(8-[3-methyl-4-[(1-methyl-1H-1,3-benzimidazol-5-yl)oxy]anilino]pyrimido[5,4-d]pyrimidin-2-yl)piperidin-4-yl]propanamide |
常见问题（FAQ）
宗艾替尼的适应症有哪些？
已批准的适应症包括：非小细胞肺癌。
宗艾替尼的专利什么时候到期？
宗艾替尼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。
宗艾替尼有几条合成路线？
本站收录 5 条合成路线，最短路线 3 步、总收率 /。每条路线的中间体均带登记编号与 CAS 号。
宗艾替尼的关键中间体在哪里可以采购？
宗艾替尼的多条路线中间体已挂接 CAS 档案，其中 4 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。
如何获取宗艾替尼中间体的报价？
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） · 2026-10-22