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普拉替尼
Tier C · 观察 / 贸易Pralsetinib · 2031 年到期全部品种 →
Blueprint Medicines Corp
原研
2020
首批上市
2031
到期年（公开口径）
$0.3B *
峰值销售
化学药
类型
靶点：RET
商品名：Pujihua、普吉华、GAVRETO、Gavreto
适应症（已批准）：非小细胞肺癌、甲状腺瘤、甲状腺髓样癌
各地区研发/上市状态
美国
批准上市
2020-09-04
欧盟
批准上市
2021-11-18
中国
批准上市
2021-03-24
日本
终止
2020-07-24
合成路线与中间体7 routes
原研路线 × 0优化路线（非专利）× 7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 8 · 总收率 /
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)1024528-1-a,(I)1024528-1-d | 4746-97-8 | 1,4 Cyclohexanedione ethylene ketal |
| (II)1024528-1-a | 2097133-36-1 | Methyl 8-methoxy-1,4-dioxaspiro[4.5]decane-8-carboxylate |
| (III)1024528-1-a | 1622928-67-9 | Methyl 1-methoxy-4-oxocyclohexane-1-carboxylate |
| (IV)1024528-1-a | 2097133-42-9 | Methyl 4-hydroxy-1-methoxycyclohexane-1-carboxylate |
| (V)1024528-1-a | 2097133-18-9 | Methyl 4-iodo-1-methoxycyclohexane-1-carboxylate |
| (VI)1024528-1-a | 89466-59-1 | 2-Chloro-4-methyl-6-(methylsulfanyl)pyrimidine |
| (VII)1024528-1-a | 5424-21-5 | 2,4-Dichloro-6-methylpyrimidine |
| (VIII)1024528-1-a | 2742918-71-2 | Methyl 1-methoxy-4-[4-methyl-6-(methylsulfanyl)pyrimidin-2-yl]cyclohexane-1-carboxylate |
| (IX)1024528-1-a | 2097133-29-2 | Methyl 4-[4-(methanesulfonyl)-6-methylpyrimidin-2-yl]-1-methoxycyclohexane-1-carboxylate |
| (X)1024528-1-a,(X)1024528-1-d | 2097133-30-5 | Methyl 1-methoxy-4-(4-methyl-6-oxo-1,6-dihydropyrimidin-2-yl)cyclohexane-1-carboxylate |
| (XI)1024528-1-a,(XI)1024528-1-b | 2097133-31-6 | Methyl 4-(4-chloro-6-methylpyrimidin-2-yl)-1-methoxycyclohexane-1-carboxylate |
优化Route 2步骤 4 · 总收率 /
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (XI)1024528-1-a,(XI)1024528-1-b | 2097133-31-6 | Methyl 4-(4-chloro-6-methylpyrimidin-2-yl)-1-methoxycyclohexane-1-carboxylate |
| (XII)1024528-1-b | 31230-17-8 | 3-Amino-5-methylpyrazole |
| (XIII)1024528-1-b | 2097133-32-7 | Methyl 1-methoxy-4-[4-methyl-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]cyclohexane-1-carboxylate |
| (XIV)1024528-1-b | 2459966-45-9 | 1-Methoxy-4-[4-methyl-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]cyclohexane-1-carboxylic acid |
| (XIX)1024528-1-b,(XIX)1024528-1-c | 1980023-94-6 | 1-[6-(4-Fluoro-1H-pyrazol-1-yl)pyridin-3-yl]ethan-1-one |
| (XV)1024528-1-b | 139042-59-4 | 1-(6-Bromopyridin-3-yl)ethan-1-one |
| (XVa)1024528-1-b | 2097133-17-8 | (1S)-1-[6-(4-Fluoro-1H-pyrazol-1-yl)pyridin-3-yl]ethan-1-amine hydrogen chloride |
| (XVb)1024528-1-b | 1980023-96-8 | (1S)-1-[6-(4-Fluoro-1H-pyrazol-1-yl)pyridin-3-yl]ethan-1-amine |
| (XVc)1024528-1-b | - | (1S)-1-[6-(4-Fluoro-1H-pyrazol-1-yl)pyridin-3-yl]ethan-1-amine hydrogen chloride (1/2) |
| (XVII)1024528-1-b,(XVII)1024528-1-c | 35277-02-2 | 4-Fluoro-1H-pyrazole |
| (XVIII)1024528-1-b | 102-52-3 | 1,1,3,3-Tetrakis(methyloxy)propane |
| (XX)1024528-1-b | 196929-78-9 | (R)-(+)-2-Methyl-2-propanesulfinamide |
| (XXI)1024528-1-b | 1980023-95-7 | (SR)-N-[(1S)-1-[6-(4-Fluoro-1H-pyrazol-1-yl)pyridin-3-yl]ethyl]-2-methylpropane-2-sulfinamide |
优化Route 3步骤 7 · 总收率 /
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (XIX)1024528-1-b,(XIX)1024528-1-c | 1980023-94-6 | 1-[6-(4-Fluoro-1H-pyrazol-1-yl)pyridin-3-yl]ethan-1-one |
| (XVII)1024528-1-b,(XVII)1024528-1-c | 35277-02-2 | 4-Fluoro-1H-pyrazole |
| (XXII)1024528-1-c | 76-37-9 | 2,2,3,3-Tetrafluoropropan-1-ol |
| (XXIII)1024528-1-c | 343331-58-8 | 4-(2,2,3,3-Tetrafluoropropyl)morpholine |
| (XXIV)1024528-1-c | 1438425-76-3 | 4-Methyl-4-(2,2,3,3-tetrafluoropropyl)morpholin-4-ium mesylate |
| (XXIX)1024528-1-c | 288-13-1在售 | 1,2-Diazole |
| (XXV)1024528-1-c | - | 4-Methyl-4-[(1Z)-2,3,3-trifluoroprop-1-en-1-yl]morpholin-4-ium methanesulfonate |
| (XXVI)1024528-1-c | - | (2Z)-2-Fluoro-3-(morpholin-4-yl)prop-2-enal |
| (XXVII)1024528-1-c | 5341-61-7 | Hydrazine dihydrochloride |
| (XXVIII)1024528-1-c | - | 4-Fluoro-1H-pyrazole hydrogen chloride |
| (XXX)1024528-1-c | 53939-30-3 | 5-Bromo-2-chloropyridine |
| (XXXI)1024528-1-c | 108-24-7 | Acetic acid acetic anhydride |
| (XXXII)1024528-1-c | 55676-22-7 | 1-(6-Chloropyridin-3-yl)ethanone |
优化Route 4步骤 6 · 总收率 /
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)1024528-1-a,(I)1024528-1-d | 4746-97-8 | 1,4 Cyclohexanedione ethylene ketal |
| (X)1024528-1-a,(X)1024528-1-d | 2097133-30-5 | Methyl 1-methoxy-4-(4-methyl-6-oxo-1,6-dihydropyrimidin-2-yl)cyclohexane-1-carboxylate |
| (XXXIII)1024528-1-d | 69947-09-7 | 1,4-Dioxaspiro[4.5]decane-8-carbonitrile |
| (XXXIV)1024528-1-d | 1252690-12-2 | N-Hydroxy-1,4-dioxaspiro[4.5]decane-8-carboximidamide |
| (XXXV)1024528-1-d | 1252973-00-4 | 1,4-Dioxaspiro[4.5]decane-8-carboximidamide |
| (XXXVI)1024528-1-d | 141-97-9在售 | 1-Ethoxybutane-1,3-dione |
| (XXXVII)1024528-1-d | - | 2-(1,4-Dioxaspiro[4.5]decan-8-yl)-6-methylpyrimidin-4-ol |
| (XXXVIII)1024528-1-d | - | 4-(4-Hydroxy-6-methylpyrimidin-2-yl)cyclohexan-1-one |
优化Route 5步骤 5 · 总收率 /
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)1024528-2-a | 14394-60-6 | 2-Chloro-6-methylpyrimidin-4-amine |
| (II)1024528-2-a | 2675521-17-0 | tert-Butyl (2-chloro-6-methylpyrimidin-4-yl)carbamate |
| (III)1024528-2-a | 2097133-18-9 | Methyl 4-iodo-1-methoxycyclohexane-1-carboxylate |
| (IV)1024528-2-a | 2675521-16-9 | Methyl 4-[4-[(tert-butoxycarbonyl)amino]-6-methylpyrimidin-2-yl]-1-methoxycyclohexane-1-carboxylate |
| (V)1024528-2-a | 2097133-30-5 | Methyl 1-methoxy-4-(4-methyl-6-oxo-1,6-dihydropyrimidin-2-yl)cyclohexane-1-carboxylate |
| (VI)1024528-2-a | 578008-32-9 | 3-Amino-1-Boc-5-methyl-1H-pyrazole |
| (VII)1024528-2-a | 2097133-32-7 | Methyl 1-methoxy-4-[4-methyl-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]cyclohexane-1-carboxylate |
| (VIII)1024528-2-a | 1980023-96-8 | (1S)-1-[6-(4-Fluoro-1H-pyrazol-1-yl)pyridin-3-yl]ethan-1-amine |
优化Route 6步骤 7 · 总收率 /
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)1024528-3-a,(I)1024528-3-b | 2778223-41-7 | Methyl 4-cyano-1-methoxycyclohexane-1-carboxylate |
| (II)1024528-3-a | - | Methyl 4-[imino(methoxy)methyl]-1-methoxycyclohexane-1-carboxylate hydrogen chloride |
| (III)1024528-3-a | - | Methyl trans-4-carbamimidoyl-1-methoxycyclohexane-1-carboxylate |
| (IV)1024528-3-a | 105-45-3在售 | 1-Methoxybutane-1,3-dione |
| (V)1024528-3-a | 2097133-30-5 | Methyl 1-methoxy-4-(4-methyl-6-oxo-1,6-dihydropyrimidin-2-yl)cyclohexane-1-carboxylate |
| (VI)1024528-3-a | - | Methyl trans-4-[4-[(methanesulfonyl)oxy]-6-methylpyrimidin-2-yl]-1-methoxycyclohexane-1-carboxylate |
| (VII)1024528-3-a | 31230-17-8 | 3-Amino-5-methylpyrazole |
| (VIII)1024528-3-a | - | Methyl (1s,4s)-1-methoxy-4-[4-methyl-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]cyclohexane-1-carboxylate |
| (IX)1024528-3-a | - | (1s,4s)-1-Methoxy-4-[4-methyl-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]cyclohexane-1-carboxylic acid |
| (Xa)1024528-3-a | 1980023-96-8 | (1S)-1-[6-(4-Fluoro-1H-pyrazol-1-yl)pyridin-3-yl]ethan-1-amine |
| (Xb)1024528-3-a | 2097133-17-8 | (1S)-1-[6-(4-Fluoro-1H-pyrazol-1-yl)pyridin-3-yl]ethan-1-amine hydrogen chloride |
优化Route 7步骤 3 · 总收率 /
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I)1024528-3-a,(I)1024528-3-b | 2778223-41-7 | Methyl 4-cyano-1-methoxycyclohexane-1-carboxylate |
| (Xb)1024528-3-a | 2097133-17-8 | (1S)-1-[6-(4-Fluoro-1H-pyrazol-1-yl)pyridin-3-yl]ethan-1-amine hydrogen chloride |
| (XI)1024528-3-b | 4746-97-8 | 1,4 Cyclohexanedione ethylene ketal |
| (XII)1024528-3-b | 2097133-36-1 | Methyl 8-methoxy-1,4-dioxaspiro[4.5]decane-8-carboxylate |
| (XIII)1024528-3-b | 1622928-67-9 | Methyl 1-methoxy-4-oxocyclohexane-1-carboxylate |
| (XIV)1024528-3-b | 69947-09-7 | 1,4-Dioxaspiro[4.5]decane-8-carbonitrile |
| (XV)1024528-3-b | 34916-10-4 | 4-Oxocyclohexane-1-carbonitrile |
常见问题（FAQ）
普拉替尼的适应症有哪些？
已批准的适应症包括：非小细胞肺癌、甲状腺瘤、甲状腺髓样癌。
普拉替尼的专利什么时候到期？
按公开口径，普拉替尼的专利到期年为 2031 年。
普拉替尼有几条合成路线？
本站收录 7 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。
普拉替尼的关键中间体在哪里可以采购？
普拉替尼的多条路线中间体已挂接 CAS 档案，其中 3 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。
如何获取普拉替尼中间体的报价？
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