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甲磺酸奥希替尼

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Osimertinib Mesylate · all drugs expiring in 2031 →

阿斯利康
Originator
2015
First approval
2031
Expiry (public)
$7.25B ▲
Peak sales
化学药
Type

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

Brand：Tagrisso、泰瑞沙

Indications (approved)：非小细胞肺癌

Regional status

US
批准上市
2015-11-13
EU
批准上市
2016-02-01
China
批准上市
2017-03-22
Japan
批准上市
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: 非小细胞肺癌.

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) · 2026-09-24