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Osimertinib Mesylate

Tier A — Act now

Osimertinib Mesylate · all drugs expiring in 2031 →

AstraZeneca
Originator
2015
First approval
2031
Expiry (public)
$7.25B ▲
Peak sales
Small molecule
Type

Targets：EGFR, HER2, HER3, HER4, EGFR T790M, EGFR L858R, EGFR 19del

Brand：Tagrisso

Indications (approved)：Non-small cell lung cancer

Regional status

US
Approved
2015-11-13
EU
Approved
2016-02-01
China
Approved
2017-03-22
Japan
Approved
2016-03-28

Synthetic routes & intermediates4 routes

Originator routes × 1Optimised (non-patent) × 3Process 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 7 · Total yield 4.9 g
Synthetic routes & intermediates Route 1
CodeCAS No.Intermediate
OSIM-001120-72-9Available1H-indole
OSIM-0023934-20-1Available2,4-dichloropyrimidine
OSIM-003945016-63-7Available3-(2-chloropyrimidin-4-yl)-1H-indole
OSIM-0041032452-86-0Available3-(2-chloropyrimidin-4-yl)-1-methyl-1H-indole
OSIM-0051075705-01-9Available4-fluoro-2-methoxy-5-nitroaniline
OSIM-0061421372-94-2AvailableN-(4-fluoro-2-methoxy-5-nitrophenyl)-4-(1-methyl-1H-indol-3-yl)pyrimidin-2-amine
OSIM-007142-25-6AvailableN1,N1,N2-trimethylethane-1,2-diamine
OSIM-0081421372-67-9AvailableN1-(2-(dimethylamino)ethyl)-5-methoxy-N1-methyl-N4-(4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)-2-nitrobenzene-1,4-diamine
OSIM-0091421372-66-8AvailableN1-(2-(dimethylamino)ethyl)-5-methoxy-N1-methyl-N4-(4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)benzene-1,2,4-triamine
OSIM-010814-68-6Availableacryloyl chloride
OSIM-01175-75-2Availablemethanesulfonic acid
OptimisedRoute 2Steps 7 · Total yield 20.5 g
Synthetic routes & intermediates Route 2
CodeCAS No.Intermediate
OSIM-0023934-20-1Available2,4-dichloropyrimidine
OSIM-0041032452-86-0Available3-(2-chloropyrimidin-4-yl)-1-methyl-1H-indole
OSIM-0051075705-01-9Available4-fluoro-2-methoxy-5-nitroaniline
OSIM-0061421372-94-2AvailableN-(4-fluoro-2-methoxy-5-nitrophenyl)-4-(1-methyl-1H-indol-3-yl)pyrimidin-2-amine
OSIM-007142-25-6AvailableN1,N1,N2-trimethylethane-1,2-diamine
OSIM-0081421372-67-9AvailableN1-(2-(dimethylamino)ethyl)-5-methoxy-N1-methyl-N4-(4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)-2-nitrobenzene-1,4-diamine
OSIM-0091421372-66-8AvailableN1-(2-(dimethylamino)ethyl)-5-methoxy-N1-methyl-N4-(4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)benzene-1,2,4-triamine
OSIM-01175-75-2Availablemethanesulfonic acid
OSIM-012603-76-9Available1-methyl-1H-indole
OSIM-013625-36-5Available3-chloropropanoyl chloride
OSIM-0141421373-36-5Available3-chloro-N-(2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)propanamide
OptimisedRoute 3Steps 5 · Total yield 190.5 mg
Synthetic routes & intermediates Route 3
CodeCAS No.Intermediate
OSIM-0041032452-86-0Available3-(2-chloropyrimidin-4-yl)-1-methyl-1H-indole
OSIM-0051075705-01-9Available4-fluoro-2-methoxy-5-nitroaniline
OSIM-007142-25-6AvailableN1,N1,N2-trimethylethane-1,2-diamine
OSIM-010814-68-6Availableacryloyl chloride
OSIM-0151802924-13-5Availabletert-butyl (4-fluoro-2-methoxy-5-nitrophenyl)carbamate
OSIM-0161802924-14-6Availabletert-butyl (4-((2-(dimethylamino)ethyl)(methyl)amino)-2-methoxy-5-nitrophenyl)carbamate
OSIM-0171802924-15-7Availabletert-butyl (5-amino-4-((2-(dimethylamino)ethyl)(methyl)amino)-2-methoxyphenyl)carbamate
OSIM-0181802924-16-8AvailableN-(5-amino-2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxyphenyl)acrylamide
OptimisedRoute 4Steps 10 · Total yield 4.55 g
Synthetic routes & intermediates Route 4
CodeCAS No.Intermediate
OSIM-007142-25-6AvailableN1,N1,N2-trimethylethane-1,2-diamine
OSIM-010814-68-6Availableacryloyl chloride
OSIM-0181802924-16-8AvailableN-(5-amino-2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxyphenyl)acrylamide
OSIM-01929632-74-4Available2-fluoro-4-iodoaniline
OSIM-020110-13-4Availablehexane-2,5-dione
OSIM-021217314-30-2Available1-(2-fluoro-4-iodophenyl)-2,5-dimethyl-1H-pyrrole
OSIM-022217314-31-3Available1-(2-fluoro-4-methoxyphenyl)-2,5-dimethyl-1H-pyrrole
OSIM-023458-52-6Available2-fluoro-4-methoxyaniline
OSIM-0241810048-26-0AvailableN-(2-fluoro-4-methoxyphenyl)acrylamide
OSIM-0251810048-27-1AvailableN-(2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxyphenyl)acrylamide
OSIM-0261810048-28-2AvailableN-(2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxy-5-nitrophenyl)acrylamide
OSIM-0271810048-29-3AvailableN-(2-((2-(dimethylamino)ethyl)(methyl)amino)-5-guanidino-4-methoxyphenyl)acrylamide
OSIM-028954421-16-0Available(E)-3-(dimethylamino)-1-(1-methyl-1H-indol-3-yl)prop-2-en-1-one
OSIM-02919012-02-3Available1-(1-methyl-1H-indol-3-yl)ethanone

Frequently asked questions

What are the approved indications of Osimertinib Mesylate?

Approved indications include: Non-small cell lung cancer.

When does the Osimertinib Mesylate patent expire?

Based on public sources, the Osimertinib Mesylate patent expires in 2031.

How many synthesis routes are recorded for Osimertinib Mesylate?

4 synthesis routes are recorded; the shortest is 5 steps with 190.5 mg total yield. Intermediates in each route carry codes and CAS numbers.

Where can I buy Osimertinib Mesylate intermediates?

29 intermediate CAS of Osimertinib Mesylate 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 Osimertinib Mesylate 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) · 2026-09-29