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阿昔替尼

Tier B — Position early

Axitinib

辉瑞
Originator
2012
First approval
-
Expiry (public)
$1.04B ▲
Peak sales
化学药
Type

Targets：VEGFR1、VEGFR3、PDGFR、VEGFR2

Brand：Inlyta、英立达

Indications (approved)：肾细胞癌

Regional status

US
批准上市
2012-01-27
EU
批准上市
2012-09-03
China
批准上市
2015-04-29
Japan
批准上市
2012-06-29

Synthetic routes & intermediates5 routes

Originator routes × 1Optimised (non-patent) × 2Process routes × 2

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 2Steps 11 · Total yield /
Synthetic routes & intermediates Route 2
CodeCAS No.Intermediate
AXIT-0017597-18-4Available6-nitro-1H-indazole
AXIT-00270315-70-7Available3-iodo-6-nitro-1H-indazole
AXIT-010319472-83-8Available3-iodo-6-nitro-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazole
AXIT-0114363-35-3Available(E)-styrylboronic acid
AXIT-012319472-84-9Available(E)-6-nitro-3-styryl-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazole
AXIT-013319472-85-0Available(E)-3-styryl-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazol-6-amine
AXIT-014319472-91-8Available(E)-6-iodo-3-styryl-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazole
AXIT-015319473-95-5Available6-iodo-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazole-3-carbaldehyde
AXIT-01638700-15-1Availabletriphenyl(pyridin-2-ylmethyl)phosphonium chloride
AXIT-017319473-96-6Available(E)-6-iodo-3-(2-(pyridin-2-yl)vinyl)-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazole
AXIT-0184892-02-8Availablemethyl 2-mercaptobenzoate
AXIT-019319473-97-7Availablemethyl (E)-2-((3-(2-(pyridin-2-yl)vinyl)-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazol-6-yl)thio)benzoate
AXIT-020319473-98-8Available(E)-2-((3-(2-(pyridin-2-yl)vinyl)-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazol-6-yl)thio)benzoic acid
AXIT-021319473-99-9Available(E)-N-methyl-2-((3-(2-(pyridin-2-yl)vinyl)-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indazol-6-yl)thio)benzamide
OptimisedRoute 4Steps 3 · Total yield /
Synthetic routes & intermediates Route 4
CodeCAS No.Intermediate
AXIT-024885126-34-1Available2-((3-iodo-1H-indazol-6-yl)thio)-N-methylbenzamide
AXIT-0251945-84-2Available2-ethynylpyridine
AXIT-026885126-38-5AvailableN-methyl-2-((3-(pyridin-2-ylethynyl)-1H-indazol-6-yl)thio)benzamide
AXIT-027885126-40-9Available(Z)-N-methyl-2-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)benzamide
OptimisedRoute 5Steps 3 · Total yield 0.82 g
Synthetic routes & intermediates Route 5
CodeCAS No.Intermediate
AXIT-00820054-45-9Available2-mercapto-N-methylbenzamide
AXIT-028115666-47-2Available6-iodo-1H-indole
AXIT-029885518-80-9Available6-iodo-1H-indazole-3-carbaldehyde
AXIT-0301487411-82-4Available2-((3-formyl-1H-indazol-6-yl)thio)-N-methylbenzamide
AXIT-03173870-22-1Availabletriphenyl(pyridin-2-ylmethyl)phosphonium bromide
ProcessRoute 1Steps 7 · Total yield 17.8 kg
Synthetic routes & intermediates Route 1
CodeCAS No.Intermediate
AXIT-0017597-18-4Available6-nitro-1H-indazole
AXIT-00270315-70-7Available3-iodo-6-nitro-1H-indazole
AXIT-003886230-74-6Available3-iodo-6-nitro-1-(tetrahydro-2H-pyran-2-yl)-1H-indazole
AXIT-004100-69-6Available2-vinylpyridine
AXIT-005886230-75-7Available(E)-6-nitro-3-(2-(pyridin-2-yl)vinyl)-1-(tetrahydro-2H-pyran-2-yl)-1H-indazole
AXIT-006886230-76-8Available(E)-3-(2-(pyridin-2-yl)vinyl)-1-(tetrahydro-2H-pyran-2-yl)-1H-indazol-6-amine
AXIT-007886230-77-9Available(E)-6-iodo-3-(2-(pyridin-2-yl)vinyl)-1-(tetrahydro-2H-pyran-2-yl)-1H-indazole
AXIT-00820054-45-9Available2-mercapto-N-methylbenzamide
AXIT-009885126-35-2Available(E)-N-methyl-2-((3-(2-(pyridin-2-yl)vinyl)-1-(tetrahydro-2H-pyran-2-yl)-1H-indazol-6-yl)thio)benzamide
ProcessRoute 3Steps 3 · Total yield 28 kg
Synthetic routes & intermediates Route 3
CodeCAS No.Intermediate
AXIT-004100-69-6Available2-vinylpyridine
AXIT-00820054-45-9Available2-mercapto-N-methylbenzamide
AXIT-022261953-36-0Available6-iodo-1H-indazole
AXIT-023944835-85-2Available2-((1H-indazol-6-yl)thio)-N-methylbenzamide
AXIT-024885126-34-1Available2-((3-iodo-1H-indazol-6-yl)thio)-N-methylbenzamide

Frequently asked questions

What are the approved indications of Axitinib?

Approved indications include: 肾细胞癌.

When does the Axitinib patent expire?

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

How many synthesis routes are recorded for Axitinib?

5 synthesis routes are recorded; the shortest is 3 steps with 28 kg total yield. Intermediates in each route carry codes and CAS numbers.

Where can I buy Axitinib intermediates?

31 intermediate CAS of Axitinib 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 Axitinib 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