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哌柏西利
Tier A — Act nowPalbociclib · all drugs expiring in 2027 →
辉瑞
Originator
2015
First approval
2027
Expiry (public)
$5.44B ▲
Peak sales
化学药
Type
Targets：CDK6、CDK4
Brand：爱博新、IBRANCE、Ibrance
Indications (approved)：乳腺癌
Regional status
US
批准上市
2015-02-03
EU
批准上市
2016-11-09
China
批准上市
2018-07-31
Japan
批准上市
2017-09-27
Synthetic routes & intermediates5 routes
Originator routes × 1Optimised (non-patent) × 4Process routes × 0
Routes are ordered originator first, then optimised / process (non-patent) routes; each lists steps, overall yield and the intermediate table (code / CAS / name) — ready for supplier sourcing and RFQ. Rendered by this site from structured data; no third-party route graphics used.
OriginatorRoute 1Steps 9 · Total yield 1.96 kg
| Code | CAS No. | Intermediate |
|---|---|---|
| PALB-012 | 57260-71-6Available | tert-butyl piperazine-1-carboxylate |
| PALB-013 | 571189-16-7Available | tert-butyl 4-(6-nitropyridin-3-yl)piperazine-1-carboxylate |
| PALB-001 | 36082-50-5Available | 5-bromo-2,4-dichloropyrimidine |
| PALB-002 | 1003-03-8Available | cyclopentanamine |
| PALB-003 | 733039-20-8Available | 5-bromo-2-chloro-N-cyclopentylpyrimidin-4-amine |
| PALB-004 | 107-93-7Available | (E)-but-2-enoic acid |
| PALB-005 | 1013916-37-4Available | 2-chloro-8-cyclopentyl-5-methylpyrido[2,3-d]pyrimidin-7(8H)-one |
| PALB-006 | 1016636-76-2Available | 6-bromo-2-chloro-8-cyclopentyl-5-methylpyrido[2,3-d]pyrimidin-7(8H)-one |
| PALB-007 | 571188-59-5Available | tert-butyl 4-(6-aminopyridin-3-yl)piperazine-1-carboxylate |
| PALB-008 | 571188-82-4Available | 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 | 111-34-2Available | 1-(vinyloxy)butane |
| PALB-010 | 866084-31-3Available | 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 | 39856-50-3Available | 5-bromo-2-nitropyridine |
OptimisedRoute 2Steps 11 · Total yield 4.01 g
| Code | CAS No. | Intermediate |
|---|---|---|
| PALB-002 | 1003-03-8Available | cyclopentanamine |
| PALB-007 | 571188-59-5Available | tert-butyl 4-(6-aminopyridin-3-yl)piperazine-1-carboxylate |
| PALB-008 | 571188-82-4Available | 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 | 5909-24-0Available | ethyl 4-chloro-2-(methylthio)pyrimidine-5-carboxylate |
| PALB-015 | 211245-62-4Available | ethyl 4-(cyclopentylamino)-2-(methylthio)pyrimidine-5-carboxylate |
| PALB-016 | 211245-63-5Available | (4-(cyclopentylamino)-2-(methylthio)pyrimidin-5-yl)methanol |
| PALB-017 | 211245-64-6Available | 4-(cyclopentylamino)-2-(methylthio)pyrimidine-5-carbaldehyde |
| PALB-018 | 362656-31-3Available | 1-(4-(cyclopentylamino)-2-(methylthio)pyrimidin-5-yl)ethanol |
| PALB-019 | 362656-11-9Available | 1-(4-(cyclopentylamino)-2-(methylthio)pyrimidin-5-yl)ethan-1-one |
| PALB-020 | 867-13-0Available | ethyl 2-(diethoxyphosphoryl)acetate |
| PALB-021 | 362656-23-3Available | 8-cyclopentyl-5-methyl-2-(methylthio)pyrido[2,3-d]pyrimidin-7(8H)-one |
| PALB-022 | 362656-25-5Available | 6-bromo-8-cyclopentyl-5-methyl-2-(methylthio)pyrido[2,3-d]pyrimidin-7(8H)-one |
| PALB-023 | 63160-15-6Available | 2-((4-nitrophenyl)sulfonyl)-3-phenyl-1,2-oxaziridine |
| PALB-024 | 571188-81-3Available | 6-bromo-8-cyclopentyl-5-methyl-2-(methylsulfinyl)pyrido[2,3-d]pyrimidin-7(8H)-one |
| PALB-025 | 97674-02-7Available | tributyl(1-ethoxyvinyl)stannane |
| PALB-026 | 571189-10-1Available | 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 |
OptimisedRoute 3Steps 5 · Total yield 7.5 g
| Code | CAS No. | Intermediate |
|---|---|---|
| PALB-002 | 1003-03-8Available | cyclopentanamine |
| PALB-007 | 571188-59-5Available | tert-butyl 4-(6-aminopyridin-3-yl)piperazine-1-carboxylate |
| PALB-027 | 141-97-9Available | ethyl 3-oxobutanoate |
| PALB-028 | 1695530-90-5Available | N-cyclopentyl-3-oxo-N-(3-oxobutanoyl)butanamide |
| PALB-029 | 1695530-92-7Available | 3-acetyl-1-cyclopentyl-6-hydroxy-4-methylpyridin-2(1H)-one |
| PALB-030 | 1695530-94-9Available | 5-acetyl-2-chloro-1-cyclopentyl-4-methyl-6-oxo-1,6-dihydropyridine-3-carbaldehyde |
| PALB-031 | 1695531-28-2Available | tert-butyl 4-(6-guanidinopyridin-3-yl)piperazine-1-carboxylate sulfate |
| PALB-032 | 14527-26-5Available | methyl carbamimidothioate sulfate |
OptimisedRoute 4Steps 9 · Total yield 24 g
| Code | CAS No. | Intermediate |
|---|---|---|
| PALB-002 | 1003-03-8Available | cyclopentanamine |
| PALB-007 | 571188-59-5Available | tert-butyl 4-(6-aminopyridin-3-yl)piperazine-1-carboxylate |
| PALB-033 | 3177-24-0Available | 2,4-dichloropyrimidine-5-carbonitrile |
| PALB-034 | 871254-62-5Available | 1-(2,4-dichloropyrimidin-5-yl)ethanone |
| PALB-035 | 1777821-88-1Available | 2,4-dichloro-5-(2-methyl-1,3-dioxolan-2-yl)pyrimidine |
| PALB-036 | 1244949-62-9Available | 1-(2-chloro-4-(cyclopentylamino)pyrimidin-5-yl)ethanone |
| PALB-037 | 674-82-8Available | 4-methyleneoxetan-2-one |
| PALB-038 | 1777821-89-2Available | N-(5-acetyl-2-chloropyrimidin-4-yl)-N-cyclopentyl-3-oxobutanamide |
| PALB-039 | 1651214-73-1Available | 6-acetyl-2-chloro-8-cyclopentyl-5-methylpyrido[2,3-d]pyrimidin-7(8H)-one |
| PALB-040 | 1777821-90-5Available | 2-chloro-8-cyclopentyl-5-methyl-6-(2-methyl-1,3-dioxolan-2-yl)pyrido[2,3-d]pyrimidin-7(8H)-one |
| PALB-041 | 1777821-91-6Available | 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 |
OptimisedRoute 5Steps 10 · Total yield 21.3 g
| Code | CAS No. | Intermediate |
|---|---|---|
| PALB-007 | 571188-59-5Available | tert-butyl 4-(6-aminopyridin-3-yl)piperazine-1-carboxylate |
| PALB-011 | 39856-50-3Available | 5-bromo-2-nitropyridine |
| PALB-013 | 571189-16-7Available | tert-butyl 4-(6-nitropyridin-3-yl)piperazine-1-carboxylate |
| PALB-042 | 110-85-0Available | piperazine |
| PALB-043 | 775288-71-6Available | 1-(6-nitropyridin-3-yl)piperazine |
| PALB-044 | 145013-05-4Available | - |
| PALB-045 | 909712-07-8Available | (Z)-tert-butyl 4-(6-(2,3-bis(tert-butoxycarbonyl)guanidino)pyridin-3-yl)piperazine-1-carboxylate |
| PALB-046 | 909712-05-6Available | 1-(5-(piperazin-1-yl)pyridin-2-yl)guanidine hydrochloride |
| PALB-047 | 15802-53-6Available | (E)-methyl 2-acetylbut-2-enoate |
| PALB-048 | 1838587-06-6Available | 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 | 1838587-07-7Available | 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 | 930-28-9Available | chlorocyclopentane |
| PALB-051 | 1684447-27-5Available | 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 | 105-45-3Available | methyl 3-oxobutanoate |
Frequently asked questions
What are the approved indications of Palbociclib?
Approved indications include: 乳腺癌.
When does the Palbociclib patent expire?
Based on public sources, the Palbociclib patent expires in 2027.
How many synthesis routes are recorded for Palbociclib?
5 synthesis routes are recorded; the shortest is 5 steps with 7.5 g total yield. Intermediates in each route carry codes and CAS numbers.
Where can I buy Palbociclib intermediates?
52 intermediate CAS of Palbociclib are available through the Unibest supply network — see the route tables on this page and request a quote per CAS.
How do I get a quote for Palbociclib intermediates?
Open the CAS profile of the target intermediate from this page, or submit an RFQ directly — the CAS enters the matching flow automatically and the supply network responds with quotes.
Source: cross-verified data (structured fields only) · 2026-09-24