palbociclib
Ibrance · Pfizer · CDK4/6
明确不做（太卷）门槛 3/5
- US LOE
- 2027
- 备注
- —
- 准备期
- 1 年
- 年销售
- ~$4B
- 关键中间体
- 0 个
门槛构成
多家 ANDA 2019 已报新进入者无准备期
明确不做
2027 到期 + 多家 ANDA 2019 年已报，新进入者无准备期（但核心中间体与 Kisqali 平台共享，可借 Kisqali 切入）。
关键中间体链
本目录已覆盖 0/0暂无需外销的中间体（如生物药 / 发酵源品种）。
药渡合成路线 · 中间体全表仅结构化数据（编号 / CAS / 分子式），路线由本站自行渲染
5 条路线 · 52 个节点 · 去重 CAS 52 个哌柏西利PalbociclibdrugId 86077208974879696503
原研路线 · 9 步 · 总收率 1.96 kg · 文献 WO2014128588A1 / WO2008032157A2优化路线 · 11 步 · 总收率 4.01 g · 文献 WO03062236A1 / US6936612B2优化路线 · 5 步 · 总收率 7.5 g · 文献 CN104478874A / CN104447743A优化路线 · 9 步 · 总收率 24 g · 文献 CN104610254A优化路线 · 10 步 · 总收率 21.3 g · 文献 WO2006095159A1 / CN105111205A
| 编号 | CAS 号 | 分子式 | 分子量 | 英文名 / 结构描述 |
|---|---|---|---|---|
| PALB-012 | 57260-71-6 | C9H18N2O2 | 186.26 | tert-butyl piperazine-1-carboxylate |
| PALB-013 | 571189-16-7 | C14H20N4O4 | 308.33 | tert-butyl 4-(6-nitropyridin-3-yl)piperazine-1-carboxylate |
| PALB-001 | 36082-50-5 | C4HBrCl2N2 | 227.87 | 5-bromo-2,4-dichloropyrimidine |
| PALB-002 | 1003-03-8 | C5H11N | 85.15 | cyclopentanamine |
| PALB-003 | 733039-20-8 | C9H11BrClN3 | 276.56 | 5-bromo-2-chloro-N-cyclopentylpyrimidin-4-amine |
| PALB-004 | 107-93-7 | C4H6O2 | 86.09 | (E)-but-2-enoic acid |
| PALB-005 | 1013916-37-4 | C13H14ClN3O | 263.72 | 2-chloro-8-cyclopentyl-5-methylpyrido[2,3-d]pyrimidin-7(8H)-one |
| PALB-006 | 1016636-76-2 | C13H13BrClN3O | 342.62 | 6-bromo-2-chloro-8-cyclopentyl-5-methylpyrido[2,3-d]pyrimidin-7(8H)-one |
| PALB-007 | 571188-59-5 | C14H22N4O2 | 278.35 | tert-butyl 4-(6-aminopyridin-3-yl)piperazine-1-carboxylate |
| PALB-008 | 571188-82-4 | C27H34BrN7O3 | 584.51 | 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 | C6H12O | 100.16 | 1-(vinyloxy)butane |
| PALB-010 | 866084-31-3 | C33H45N7O4 | 603.75 | 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 | C5H3BrN2O2 | 202.99 | 5-bromo-2-nitropyridine |
| PALB-014 | 5909-24-0 | C8H9ClN2O2S | 232.68 | ethyl 4-chloro-2-(methylthio)pyrimidine-5-carboxylate |
| PALB-015 | 211245-62-4 | C13H19N3O2S | 281.37 | ethyl 4-(cyclopentylamino)-2-(methylthio)pyrimidine-5-carboxylate |
| PALB-016 | 211245-63-5 | C11H17N3OS | 239.34 | (4-(cyclopentylamino)-2-(methylthio)pyrimidin-5-yl)methanol |
| PALB-017 | 211245-64-6 | C11H15N3OS | 237.32 | 4-(cyclopentylamino)-2-(methylthio)pyrimidine-5-carbaldehyde |
| PALB-018 | 362656-31-3 | C12H19N3OS | 253.36 | 1-(4-(cyclopentylamino)-2-(methylthio)pyrimidin-5-yl)ethanol |
| PALB-019 | 362656-11-9 | C12H17N3OS | 251.35 | 1-(4-(cyclopentylamino)-2-(methylthio)pyrimidin-5-yl)ethan-1-one |
| PALB-020 | 867-13-0 | C8H17O5P | 224.19 | ethyl 2-(diethoxyphosphoryl)acetate |
| PALB-021 | 362656-23-3 | C14H17N3OS | 275.37 | 8-cyclopentyl-5-methyl-2-(methylthio)pyrido[2,3-d]pyrimidin-7(8H)-one |
| PALB-022 | 362656-25-5 | C14H16BrN3OS | 354.27 | 6-bromo-8-cyclopentyl-5-methyl-2-(methylthio)pyrido[2,3-d]pyrimidin-7(8H)-one |
| PALB-023 | 63160-15-6 | C13H10N2O5S | 306.29 | 2-((4-nitrophenyl)sulfonyl)-3-phenyl-1,2-oxaziridine |
| PALB-024 | 571188-81-3 | C14H16BrN3O2S | 370.26 | 6-bromo-8-cyclopentyl-5-methyl-2-(methylsulfinyl)pyrido[2,3-d]pyrimidin-7(8H)-one |
| PALB-025 | 97674-02-7 | C16H34OSn | 361.15 | tributyl(1-ethoxyvinyl)stannane |
| PALB-026 | 571189-10-1 | C31H41N7O4 | 575.7 | 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 |
| PALB-027 | 141-97-9 | C6H10O3 | 130.14 | ethyl 3-oxobutanoate |
| PALB-028 | 1695530-90-5 | C13H19NO4 | 253.29 | N-cyclopentyl-3-oxo-N-(3-oxobutanoyl)butanamide |
| PALB-029 | 1695530-92-7 | C13H17NO3 | 235.28 | 3-acetyl-1-cyclopentyl-6-hydroxy-4-methylpyridin-2(1H)-one |
| PALB-030 | 1695530-94-9 | C14H16ClNO3 | 281.73 | 5-acetyl-2-chloro-1-cyclopentyl-4-methyl-6-oxo-1,6-dihydropyridine-3-carbaldehyde |
| PALB-031 | 1695531-28-2 | C15H24N6O2·H2SO4 | 418.47 | tert-butyl 4-(6-guanidinopyridin-3-yl)piperazine-1-carboxylate sulfate |
| PALB-032 | 14527-26-5 | C2H8N2O4S2 | 188.23 | methyl carbamimidothioate sulfate |
| PALB-033 | 3177-24-0 | C5HCl2N3 | 173.99 | 2,4-dichloropyrimidine-5-carbonitrile |
| PALB-034 | 871254-62-5 | C6H4Cl2N2O | 191.01 | 1-(2,4-dichloropyrimidin-5-yl)ethanone |
| PALB-035 | 1777821-88-1 | C8H8Cl2N2O2 | 235.07 | 2,4-dichloro-5-(2-methyl-1,3-dioxolan-2-yl)pyrimidine |
| PALB-036 | 1244949-62-9 | C11H14ClN3O | 239.7 | 1-(2-chloro-4-(cyclopentylamino)pyrimidin-5-yl)ethanone |
| PALB-037 | 674-82-8 | C4H4O2 | 84.07 | 4-methyleneoxetan-2-one |
| PALB-038 | 1777821-89-2 | C15H18ClN3O3 | 323.77 | N-(5-acetyl-2-chloropyrimidin-4-yl)-N-cyclopentyl-3-oxobutanamide |
| PALB-039 | 1651214-73-1 | C15H16ClN3O2 | 305.76 | 6-acetyl-2-chloro-8-cyclopentyl-5-methylpyrido[2,3-d]pyrimidin-7(8H)-one |
| PALB-040 | 1777821-90-5 | C17H20ClN3O3 | 349.81 | 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 | C31H41N7O5 | 591.7 | 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 |
| PALB-042 | 110-85-0 | C4H10N2 | 86.14 | piperazine |
| PALB-043 | 775288-71-6 | C9H12N4O2 | 208.22 | 1-(6-nitropyridin-3-yl)piperazine |
| PALB-044 | 145013-05-4 | C11H20N2O4S | 276.35 | — |
| PALB-045 | 909712-07-8 | C25H40N6O6 | 520.62 | (Z)-tert-butyl 4-(6-(2,3-bis(tert-butoxycarbonyl)guanidino)pyridin-3-yl)piperazine-1-carboxylate |
| PALB-046 | 909712-05-6 | C10H16N6·HCl | 256.74 | 1-(5-(piperazin-1-yl)pyridin-2-yl)guanidine hydrochloride |
| PALB-047 | 15802-53-6 | C7H10O3 | 142.15 | (E)-methyl 2-acetylbut-2-enoate |
| PALB-048 | 1838587-06-6 | C19H24N8O2 | 396.45 | 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 | C19H23N7O2 | 381.43 | 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 | C5H9Cl | 104.58 | chlorocyclopentane |
| PALB-051 | 1684447-27-5 | C24H31N7O2 | 449.55 | 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 | C5H8O3 | 116.12 | methyl 3-oxobutanoate |
数据来源：药渡（Pharmacodia）授权账号，仅取结构化字段；本方未使用药渡的路线图（webImg）—— 其图形带水印，属第三方著作权内容，转载需授权。本表由本站依据数据自行渲染。 标注「药渡未登记」者，为药渡该节点 CAS 字段为空，非本站遗漏。
按选品与立项 SOP 复核初筛层：只用本库已有字段，客户关与商业关需人工录入
用评分器补全五关 ↗市场关 · 窗口不进
准备期 1 年 · 不足 3 年
US LOE 2027
市场关 · 峰值销售可进
≈$4B · 优先档（≥$3B）
公开口径 ~$4B
供给关 · 稀缺程度不进
供给拥挤 · 明确不做
梯队判定：明确不做（太卷）
技术关 · 门槛看情况
门槛 3/5 · 临界（需代差确认）
多家 ANDA 2019 已报 · 新进入者无准备期
客户关待录入
海外客户触达与推进阶段未入库
需 ≥1 家原研/Biotech/欧美 CDMO，且 ≥2 家进入样品测试、审计或商务谈判
商业关待录入
单吨产值、账期与产能占用未入库
按单位产能毛利排序，不按单吨价格排序；账期与库存不成立即不做
市场关与供给关、技术关的结论由本库字段机械映射得出（映射口径见SOP 第 1 节）； 客户关与商业关不在本库数据范围内，须由商务与财务按 SOP 第 2 节逐条录入后才能出立项结论。
提示：LOE 日期与门槛为公开源交叉核实结果（2026-09-13），最终以原研专利登记与 FDA / EMA 官方公告为准。 关键中间体 CAS 与合成路线来自药渡（Pharmacodia）授权账号查询，仅取结构化数据、逐条做存在性校验 （见
scripts/build-loe-routes.mjs）；标「待核实」者为尚未匹配或代码层未提供名称， 入库采纳前请再经一次人工复核。