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哌柏西利
Tier A · 立即攻坚Palbociclib · 2027 年到期全部品种 →
辉瑞
原研
2015
首批上市
2027
到期年（公开口径）
$5.44B ▲
峰值销售
化学药
类型
靶点：CDK6、CDK4
商品名：爱博新、IBRANCE、Ibrance
适应症（已批准）：乳腺癌
各地区研发/上市状态
美国
批准上市
2015-02-03
欧盟
批准上市
2016-11-09
中国
批准上市
2018-07-31
日本
批准上市
2017-09-27
合成路线与中间体5 routes
原研路线 × 1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。
原研Route 1步骤 9 · 总收率 1.96 kg
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| PALB-012 | 57260-71-6在售 | tert-butyl piperazine-1-carboxylate |
| PALB-013 | 571189-16-7在售 | tert-butyl 4-(6-nitropyridin-3-yl)piperazine-1-carboxylate |
| PALB-001 | 36082-50-5在售 | 5-bromo-2,4-dichloropyrimidine |
| PALB-002 | 1003-03-8在售 | cyclopentanamine |
| PALB-003 | 733039-20-8在售 | 5-bromo-2-chloro-N-cyclopentylpyrimidin-4-amine |
| PALB-004 | 107-93-7在售 | (E)-but-2-enoic acid |
| PALB-005 | 1013916-37-4在售 | 2-chloro-8-cyclopentyl-5-methylpyrido[2,3-d]pyrimidin-7(8H)-one |
| PALB-006 | 1016636-76-2在售 | 6-bromo-2-chloro-8-cyclopentyl-5-methylpyrido[2,3-d]pyrimidin-7(8H)-one |
| PALB-007 | 571188-59-5在售 | tert-butyl 4-(6-aminopyridin-3-yl)piperazine-1-carboxylate |
| PALB-008 | 571188-82-4在售 | tert-butyl 4-(6-((6-bromo-8-cyclopentyl-5-methyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl)amino)pyridin-3-yl)piperazine-1-carboxylate |
| PALB-009 | 111-34-2在售 | 1-(vinyloxy)butane |
| PALB-010 | 866084-31-3在售 | tert-butyl 4-(6-((6-(1-butoxyvinyl)-8-cyclopentyl-5-methyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl)amino)pyridin-3-yl)piperazine-1-carboxylate |
| PALB-011 | 39856-50-3在售 | 5-bromo-2-nitropyridine |
优化Route 2步骤 11 · 总收率 4.01 g
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| PALB-002 | 1003-03-8在售 | cyclopentanamine |
| PALB-007 | 571188-59-5在售 | tert-butyl 4-(6-aminopyridin-3-yl)piperazine-1-carboxylate |
| PALB-008 | 571188-82-4在售 | tert-butyl 4-(6-((6-bromo-8-cyclopentyl-5-methyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl)amino)pyridin-3-yl)piperazine-1-carboxylate |
| PALB-014 | 5909-24-0在售 | ethyl 4-chloro-2-(methylthio)pyrimidine-5-carboxylate |
| PALB-015 | 211245-62-4在售 | ethyl 4-(cyclopentylamino)-2-(methylthio)pyrimidine-5-carboxylate |
| PALB-016 | 211245-63-5在售 | (4-(cyclopentylamino)-2-(methylthio)pyrimidin-5-yl)methanol |
| PALB-017 | 211245-64-6在售 | 4-(cyclopentylamino)-2-(methylthio)pyrimidine-5-carbaldehyde |
| PALB-018 | 362656-31-3在售 | 1-(4-(cyclopentylamino)-2-(methylthio)pyrimidin-5-yl)ethanol |
| PALB-019 | 362656-11-9在售 | 1-(4-(cyclopentylamino)-2-(methylthio)pyrimidin-5-yl)ethan-1-one |
| PALB-020 | 867-13-0在售 | ethyl 2-(diethoxyphosphoryl)acetate |
| PALB-021 | 362656-23-3在售 | 8-cyclopentyl-5-methyl-2-(methylthio)pyrido[2,3-d]pyrimidin-7(8H)-one |
| PALB-022 | 362656-25-5在售 | 6-bromo-8-cyclopentyl-5-methyl-2-(methylthio)pyrido[2,3-d]pyrimidin-7(8H)-one |
| PALB-023 | 63160-15-6在售 | 2-((4-nitrophenyl)sulfonyl)-3-phenyl-1,2-oxaziridine |
| PALB-024 | 571188-81-3在售 | 6-bromo-8-cyclopentyl-5-methyl-2-(methylsulfinyl)pyrido[2,3-d]pyrimidin-7(8H)-one |
| PALB-025 | 97674-02-7在售 | tributyl(1-ethoxyvinyl)stannane |
| PALB-026 | 571189-10-1在售 | tert-butyl 4-(6-((8-cyclopentyl-6-(1-ethoxyvinyl)-5-methyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl)amino)pyridin-3-yl)piperazine-1-carboxylate |
优化Route 3步骤 5 · 总收率 7.5 g
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| PALB-002 | 1003-03-8在售 | cyclopentanamine |
| PALB-007 | 571188-59-5在售 | tert-butyl 4-(6-aminopyridin-3-yl)piperazine-1-carboxylate |
| PALB-027 | 141-97-9在售 | ethyl 3-oxobutanoate |
| PALB-028 | 1695530-90-5在售 | N-cyclopentyl-3-oxo-N-(3-oxobutanoyl)butanamide |
| PALB-029 | 1695530-92-7在售 | 3-acetyl-1-cyclopentyl-6-hydroxy-4-methylpyridin-2(1H)-one |
| PALB-030 | 1695530-94-9在售 | 5-acetyl-2-chloro-1-cyclopentyl-4-methyl-6-oxo-1,6-dihydropyridine-3-carbaldehyde |
| PALB-031 | 1695531-28-2在售 | tert-butyl 4-(6-guanidinopyridin-3-yl)piperazine-1-carboxylate sulfate |
| PALB-032 | 14527-26-5在售 | methyl carbamimidothioate sulfate |
优化Route 4步骤 9 · 总收率 24 g
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| PALB-002 | 1003-03-8在售 | cyclopentanamine |
| PALB-007 | 571188-59-5在售 | tert-butyl 4-(6-aminopyridin-3-yl)piperazine-1-carboxylate |
| PALB-033 | 3177-24-0在售 | 2,4-dichloropyrimidine-5-carbonitrile |
| PALB-034 | 871254-62-5在售 | 1-(2,4-dichloropyrimidin-5-yl)ethanone |
| PALB-035 | 1777821-88-1在售 | 2,4-dichloro-5-(2-methyl-1,3-dioxolan-2-yl)pyrimidine |
| PALB-036 | 1244949-62-9在售 | 1-(2-chloro-4-(cyclopentylamino)pyrimidin-5-yl)ethanone |
| PALB-037 | 674-82-8在售 | 4-methyleneoxetan-2-one |
| PALB-038 | 1777821-89-2在售 | N-(5-acetyl-2-chloropyrimidin-4-yl)-N-cyclopentyl-3-oxobutanamide |
| PALB-039 | 1651214-73-1在售 | 6-acetyl-2-chloro-8-cyclopentyl-5-methylpyrido[2,3-d]pyrimidin-7(8H)-one |
| PALB-040 | 1777821-90-5在售 | 2-chloro-8-cyclopentyl-5-methyl-6-(2-methyl-1,3-dioxolan-2-yl)pyrido[2,3-d]pyrimidin-7(8H)-one |
| PALB-041 | 1777821-91-6在售 | tert-butyl 4-(6-((8-cyclopentyl-5-methyl-6-(2-methyl-1,3-dioxolan-2-yl)-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl)amino)pyridin-3-yl)piperazine-1-carboxylate |
优化Route 5步骤 10 · 总收率 21.3 g
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| PALB-007 | 571188-59-5在售 | tert-butyl 4-(6-aminopyridin-3-yl)piperazine-1-carboxylate |
| PALB-011 | 39856-50-3在售 | 5-bromo-2-nitropyridine |
| PALB-013 | 571189-16-7在售 | tert-butyl 4-(6-nitropyridin-3-yl)piperazine-1-carboxylate |
| PALB-042 | 110-85-0在售 | piperazine |
| PALB-043 | 775288-71-6在售 | 1-(6-nitropyridin-3-yl)piperazine |
| PALB-044 | 145013-05-4在售 | - |
| PALB-045 | 909712-07-8在售 | (Z)-tert-butyl 4-(6-(2,3-bis(tert-butoxycarbonyl)guanidino)pyridin-3-yl)piperazine-1-carboxylate |
| PALB-046 | 909712-05-6在售 | 1-(5-(piperazin-1-yl)pyridin-2-yl)guanidine hydrochloride |
| PALB-047 | 15802-53-6在售 | (E)-methyl 2-acetylbut-2-enoate |
| PALB-048 | 1838587-06-6在售 | 6-acetyl-4-amino-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-5,6-dihydropyrido[2,3-d]pyrimidin-7(8H)-one |
| PALB-049 | 1838587-07-7在售 | 6-acetyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-5,6-dihydropyrido[2,3-d]pyrimidin-7(8H)-one |
| PALB-050 | 930-28-9在售 | chlorocyclopentane |
| PALB-051 | 1684447-27-5在售 | 6-acetyl-8-cyclopentyl-5-methyl-2-((5-(piperazin-1-yl)pyridin-2-yl)amino)-5,6-dihydropyrido[2,3-d]pyrimidin-7(8H)-one |
| PALB-052 | 105-45-3在售 | methyl 3-oxobutanoate |
常见问题（FAQ）
哌柏西利的适应症有哪些？
已批准的适应症包括：乳腺癌。
哌柏西利的专利什么时候到期？
按公开口径，哌柏西利的专利到期年为 2027 年。
哌柏西利有几条合成路线？
本站收录 5 条合成路线，最短路线 5 步、总收率 7.5 g。每条路线的中间体均带登记编号与 CAS 号。
哌柏西利的关键中间体在哪里可以采购？
哌柏西利的多条路线中间体已挂接 CAS 档案，其中 52 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。
如何获取哌柏西利中间体的报价？
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