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克唑替尼

Tier C — Watch / trade

Crizotinib

辉瑞
Originator
2011
First approval
-
Expiry (public)
$0.59B ▲
Peak sales
化学药
Type

Targets：ALK、ROS、MST1R、c-Met

Brand：Xalkori、赛可瑞

Indications (approved)：原发性皮肤间变性大细胞淋巴瘤、间变大细胞淋巴瘤、非小细胞肺癌

Regional status

US
批准上市
2011-08-26
EU
批准上市
2012-10-23
China
批准上市
2013-01-22
Japan
批准上市
2012-03-30

Synthetic routes & intermediates5 routes

Originator routes × 1Optimised (non-patent) × 3Process routes × 1

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 12 · Total yield 410 mg
Synthetic routes & intermediates Route 1
CodeCAS No.Intermediate
CRIT-001290835-85-7Available1-(2,6-dichloro-3-fluorophenyl)ethan-1-one
CRIT-002756520-66-8Available1-(2,6-dichloro-3-fluorophenyl)ethan-1-ol
CRIT-003877397-67-6Available1-(2,6-dichloro-3-fluorophenyl)ethyl acetate
CRIT-004877397-68-7Available(S)-1-(2,6-dichloro-3-fluorophenyl)ethyl acetate
CRIT-005877397-65-4Available(S)-1-(2,6-dichloro-3-fluorophenyl)ethan-1-ol
CRIT-00615128-82-2Available2-nitropyridin-3-ol
CRIT-007877397-70-1Available(R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-2-nitropyridine
CRIT-008877397-71-2Available(R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)pyridin-2-amine
CRIT-009877399-00-3Available(R)-5-bromo-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)pyridin-2-amine
CRIT-010877399-47-8Available-
CRIT-01173183-34-3Available4,4,4',4',5,5,5',5'-octamethyl-2,2'-bi(1,3,2-dioxaborolane)
CRIT-012877399-48-9Available-
CRIT-013877399-49-0Available(R)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridin-2-amine
CRIT-014877399-50-3Availabletert-butyl 4-(4-bromo-1H-pyrazol-1-yl)piperidine-1-carboxylate
CRIT-015877399-51-4Availabletert-butyl (R)-4-(4-(6-amino-5-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)pyridin-3-yl)-1H-pyrazol-1-yl)piperidine-1-carboxylate
OptimisedRoute 2Steps 5 · Total yield 15.34 g
Synthetic routes & intermediates Route 2
CodeCAS No.Intermediate
CRIT-009877399-00-3Available(R)-5-bromo-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)pyridin-2-amine
CRIT-01173183-34-3Available4,4,4',4',5,5,5',5'-octamethyl-2,2'-bi(1,3,2-dioxaborolane)
CRIT-015877399-51-4Availabletert-butyl (R)-4-(4-(6-amino-5-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)pyridin-3-yl)-1H-pyrazol-1-yl)piperidine-1-carboxylate
CRIT-016109384-19-2Availabletert-butyl 4-hydroxypiperidine-1-carboxylate
CRIT-017141699-59-4Availabletert-butyl 4-((methylsulfonyl)oxy)piperidine-1-carboxylate
CRIT-0183469-69-0Available4-iodo-1H-pyrazole
CRIT-019877399-73-0Availabletert-butyl 4-(4-iodo-1H-pyrazol-1-yl)piperidine-1-carboxylate
CRIT-020877399-74-1Availabletert-butyl 4-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl)piperidine-1-carboxylate
OptimisedRoute 3Steps 3 · Total yield 22.5 g
Synthetic routes & intermediates Route 3
CodeCAS No.Intermediate
CRIT-021288-13-1Available1H-pyrazole
CRIT-0227379-35-3Available4-chloropyridine hydrochloride
CRIT-0231357589-48-0Available4-(1H-pyrazol-1-yl)pyridine hydrochloride
CRIT-024762240-09-5Available4-(1H-pyrazol-1-yl)piperidine
CRIT-0251229457-94-6Available4-(4-iodo-1H-pyrazol-1-yl)piperidine
OptimisedRoute 5Steps 4 · Total yield 112 mg
Synthetic routes & intermediates Route 5
CodeCAS No.Intermediate
CRIT-005877397-65-4Available(S)-1-(2,6-dichloro-3-fluorophenyl)ethan-1-ol
CRIT-020877399-74-1Availabletert-butyl 4-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl)piperidine-1-carboxylate
CRIT-02639903-01-0Available2-amino-5-bromopyridin-3-ol
CRIT-0271207175-73-2Availabletert-butyl (5-bromo-3-hydroxypyridin-2-yl)carbamate
CRIT-0281569895-70-0Availabletert-butyl (R)-(5-bromo-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)pyridin-2-yl)carbamate
CRIT-0291569895-72-2Availabletert-butyl (R)-4-(4-(6-((tert-butoxycarbonyl)amino)-5-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)pyridin-3-yl)-1H-pyrazol-1-yl)piperidine-1-carboxylate
ProcessRoute 4Steps 1 · Total yield 20.9 kg
Synthetic routes & intermediates Route 4
CodeCAS No.Intermediate
CRIT-001290835-85-7Available1-(2,6-dichloro-3-fluorophenyl)ethan-1-one
CRIT-005877397-65-4Available(S)-1-(2,6-dichloro-3-fluorophenyl)ethan-1-ol

Frequently asked questions

What are the approved indications of Crizotinib?

Approved indications include: 原发性皮肤间变性大细胞淋巴瘤, 间变大细胞淋巴瘤, 非小细胞肺癌.

When does the Crizotinib patent expire?

No public expiry year is available for Crizotinib yet; this page updates once verified.

How many synthesis routes are recorded for Crizotinib?

5 synthesis routes are recorded; the shortest is 1 steps with 20.9 kg total yield. Intermediates in each route carry codes and CAS numbers.

Where can I buy Crizotinib intermediates?

29 intermediate CAS of Crizotinib 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 Crizotinib 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