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Linezolid

Tier B — Position early

Linezolid

Pfizer Inc.
Originator
2000
First approval
-
Expiry (public)
$1.35B ▲
Peak sales
Small molecule
Type

Targets:50S ribosomal subunit

Brand:Zolodine, Zyvoxam, Zyvoxid, Zyvoxa, Zyvox

Indications (approved):非复杂性皮肤和皮肤结构感染, Pneumonia, Complicated skin and skin structure infection, Bacteraemia, Bacterial infection, Healthcare-associated pneumonia, Infectious disease, Staphylococcal infection

Regional status

US
Approved
2000-04-18
EU
Discontinued
2001-12-01
China
Approved
2006-09-12
Japan
Approved
2001-04-04

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 7 · Total yield /
LINE-001369-34-6LINE-002110-91-8LINE-0032689-39-6LINE-00493246-53-8LINE-005168828-81-7LINE-00660456-26-0LINE-007168828-82-8LINE-008174649-09-3LINE-009168828-84-0API · Linezolid
CodeCAS No.Intermediate
LINE-001369-34-61,2-difluoro-4-nitrobenzene
LINE-002110-91-8Availablemorpholine
LINE-0032689-39-64-(2-fluoro-4-nitrophenyl)morpholine
LINE-00493246-53-83-fluoro-4-morpholinoaniline
LINE-005168828-81-7benzyl (3-fluoro-4-morpholinophenyl)carbamatebenzyl (3-fluoro-4-morpholinophenyl)carbamate
LINE-00660456-26-0Available(R)-oxiran-2-ylmethyl butyrate
LINE-007168828-82-8(R)-3-(3-fluoro-4-morpholinophenyl)-5-(hydroxymethyl)oxazolidin-2-one
LINE-008174649-09-3(R)-(3-(3-fluoro-4-morpholinophenyl)-2-oxooxazolidin-5-yl)methyl methanesulfonate
LINE-009168828-84-0(R)-5-(azidomethyl)-3-(3-fluoro-4-morpholinophenyl)oxazolidin-2-one
OptimisedRoute 2Steps 8 · Total yield 1.75 g
LINE-00493246-53-8LINE-0105736-03-8LINE-0115736-03-8LINE-012541-41-3LINE-0131088110-89-7LINE-0141088110-90-0LINE-0151088110-91-1LINE-0161088110-92-2LINE-0171088110-93-3LINE-0181088110-97-7LINE-0191088111-01-6API · Linezolid
CodeCAS No.Intermediate
LINE-00493246-53-83-fluoro-4-morpholinoaniline
LINE-0105736-03-8N-((2,2-dimethyl-1,3-dioxolan-4-yl)methyl)-3-fluoro-4-morpholinoaniline
LINE-0115736-03-8N-((2,2-dimethyl-1,3-dioxolan-4-yl)methyl)-3-fluoro-4-morpholinoaniline
LINE-012541-41-3ethyl carbonochloridate
LINE-0131088110-89-7ethyl ((2,2-dimethyl-1,3-dioxolan-4-yl)methyl)(3-fluoro-4-morpholinophenyl)carbamate
LINE-0141088110-90-0ethyl (2,3-dihydroxypropyl)(3-fluoro-4-morpholinophenyl)carbamate
LINE-0151088110-91-1ethyl (3-fluoro-4-morpholinophenyl)(2-oxoethyl)carbamate
LINE-0161088110-92-2(R)-N-((R)-1-hydroxy-4-methyl-1,1-diphenylpentan-2-yl)pyrrolidine-2-carboxamide
LINE-0171088110-93-3ethyl (S)-(3-fluoro-4-morpholinophenyl)(2-hydroxy-4-oxopentyl)carbamate
LINE-0181088110-97-7ethyl (S,E)-(3-fluoro-4-morpholinophenyl)(2-hydroxy-4-(hydroxyimino)pentyl)carbamate
LINE-0191088111-01-6(S,E)-3-(3-fluoro-4-morpholinophenyl)-5-(2-(hydroxyimino)propyl)oxazolidin-2-one
OptimisedRoute 3Steps 6 · Total yield 0.92 g
LINE-001369-34-6LINE-002110-91-8LINE-0032689-39-6LINE-00493246-53-8LINE-009168828-84-0LINE-020224323-51-7LINE-02151594-55-9LINE-022496031-57-3API · Linezolid
CodeCAS No.Intermediate
LINE-001369-34-61,2-difluoro-4-nitrobenzene
LINE-002110-91-8Availablemorpholine
LINE-0032689-39-64-(2-fluoro-4-nitrophenyl)morpholine
LINE-00493246-53-83-fluoro-4-morpholinoaniline
LINE-009168828-84-0(R)-5-(azidomethyl)-3-(3-fluoro-4-morpholinophenyl)oxazolidin-2-one
LINE-020224323-51-74-(2-fluoro-4-isocyanatophenyl)morpholine
LINE-02151594-55-9(R)-2-(chloromethyl)oxirane
LINE-022496031-57-3(R)-5-(chloromethyl)-3-(3-fluoro-4-morpholinophenyl)oxazolidin-2-one
OptimisedRoute 4Steps 6 · Total yield 8.50 g
LINE-00493246-53-8LINE-009168828-84-0LINE-02367843-74-7LINE-024681225-50-3LINE-025681225-56-9LINE-0261571118-50-7LINE-027168828-90-8API · Linezolid
CodeCAS No.Intermediate
LINE-00493246-53-83-fluoro-4-morpholinoaniline
LINE-009168828-84-0(R)-5-(azidomethyl)-3-(3-fluoro-4-morpholinophenyl)oxazolidin-2-one
LINE-02367843-74-7Available(S)-2-(chloromethyl)oxirane
LINE-024681225-50-3Available(S)-1-azido-3-chloropropan-2-ol
LINE-025681225-56-9(R)-2-(azidomethyl)oxirane
LINE-0261571118-50-7(R)-1-azido-3-((3-fluoro-4-morpholinophenyl)amino)propan-2-ol
LINE-027168828-90-8(S)-5-(aminomethyl)-3-(3-fluoro-4-morpholinophenyl)oxazolidin-2-one
OptimisedRoute 5Steps 5 · Total yield /
LINE-028513068-89-8LINE-0297517-99-9LINE-030513068-96-7LINE-031858344-36-2LINE-0321385053-41-7LINE-0331352030-06-8API · Linezolid
CodeCAS No.Intermediate
LINE-028513068-89-84-(4-bromo-2-fluorophenyl)morpholine
LINE-0297517-99-95-(hydroxymethyl)oxazolidin-2-one
LINE-030513068-96-73-(3-fluoro-4-morpholinophenyl)-5-(hydroxymethyl)oxazolidin-2-one
LINE-031858344-36-2(3-(3-fluoro-4-morpholinophenyl)-2-oxooxazolidin-5-yl)methyl methanesulfonate
LINE-0321385053-41-75-(azidomethyl)-3-(3-fluoro-4-morpholinophenyl)oxazolidin-2-one
LINE-0331352030-06-85-(aminomethyl)-3-(3-fluoro-4-morpholinophenyl)oxazolidin-2-one

Frequently asked questions

What are the approved indications of Linezolid?

Approved indications include: 非复杂性皮肤和皮肤结构感染, Pneumonia, Complicated skin and skin structure infection, Bacteraemia, Bacterial infection, Healthcare-associated pneumonia, Infectious disease, Staphylococcal infection.

When does the Linezolid patent expire?

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

How many synthesis routes are recorded for Linezolid?

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

Where can I buy Linezolid intermediates?

4 intermediate CAS of Linezolid 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 Linezolid 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