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Nintedanib Esylate

Tier B — Position early

Nintedanib Esylate

Boehringer Ingelheim
Originator
2014
First approval
-
Expiry (public)
$2.83B ▲
Peak sales
Small molecule
Type

Targets：VEGFR1, VEGFR3, PDGFR-β, FGFR1, FGFR3, FGFR2, VEGFR2, FLT3, PDGFR-α, CSF1R

Brand：Vargatef, Ofev

Indications (approved)：Systemic sclerosis-associated interstitial lung disease, Idiopathic pulmonary fibrosis, Non-small cell lung cancer

Regional status

US
Approved
2014-10-15
EU
Approved
2014-11-21
China
Approved
2017-09-20
Japan
Approved
2015-07-03

Synthetic routes & intermediates4 routes

Originator routes × 1Optimised (non-patent) × 2Process 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 7 · Total yield 12.4 g
Synthetic routes & intermediates Route 1
CodeCAS No.Intermediate
NINT-001618-95-1Availablemethyl 3-nitrobenzoate
NINT-00296-34-4Availablemethyl 2-chloroacetate
NINT-003334952-07-7Availablemethyl 4-(2-methoxy-2-oxoethyl)-3-nitrobenzoate
NINT-00414192-26-8Availablemethyl 2-oxo-1,3-dihydroindole-6-carboxylate
NINT-005676326-36-6Availablemethyl 1-acetyl-2-oxoindoline-6-carboxylate
NINT-006707-07-3Available(trimethoxymethyl)benzene
NINT-0071253769-13-9Available(Z)-methyl 1-acetyl-3-(methoxy(phenyl)methylene)-2-oxoindoline-6-carboxylate
NINT-008262368-30-9AvailableN-(4-aminophenyl)-2-(4-methylpiperazin-1-yl)acetamide
NINT-00923543-31-9Available2-bromo-N-methyl-N-(4-nitrophenyl)acetamide
NINT-010109-01-3Available1-methylpiperazine
NINT-0111139453-98-7AvailableN-methyl-2-(4-methylpiperazin-1-yl)-N-(4-nitrophenyl)acetamide
OptimisedRoute 2Steps 10 · Total yield 35.1 g
Synthetic routes & intermediates Route 2
CodeCAS No.Intermediate
NINT-00414192-26-8Availablemethyl 2-oxo-1,3-dihydroindole-6-carboxylate
NINT-006707-07-3Available(trimethoxymethyl)benzene
NINT-008262368-30-9AvailableN-(4-aminophenyl)-2-(4-methylpiperazin-1-yl)acetamide
NINT-010109-01-3Available1-methylpiperazine
NINT-01296-99-1Available4-chloro-3-nitrobenzoic acid
NINT-01314719-83-6Availablemethyl 4-chloro-3-nitrobenzoate
NINT-014108-59-8Availabledimethyl malonate
NINT-0151160293-27-5Availabledimethyl 2-(4-(methoxycarbonyl)-2-nitrophenyl)malonate
NINT-016541-88-8Available2-chloroacetic anhydride
NINT-0171160293-25-3Availablemethyl 1-(2-chloroacetyl)-2-oxoindoline-6-carboxylate
NINT-0181160293-24-2Available(Z)-methyl 1-(2-chloroacetyl)-3-(methoxy(phenyl)methylene)-2-oxoindoline-6-carboxylate
NINT-0191160293-22-0Available(Z)-methyl 3-(methoxy(phenyl)methylene)-2-oxoindoline-6-carboxylate
NINT-020594-45-6Availableethanesulfonic acid
NINT-021100-15-2AvailableN-methyl-4-nitroaniline
NINT-02279-04-9Available2-chloroacetyl chloride
NINT-0232653-16-9Available2-chloro-N-methyl-N-(4-nitrophenyl)acetamide
OptimisedRoute 3Steps 3 · Total yield 2.37 g
Synthetic routes & intermediates Route 3
CodeCAS No.Intermediate
NINT-003334952-07-7Availablemethyl 4-(2-methoxy-2-oxoethyl)-3-nitrobenzoate
NINT-006707-07-3Available(trimethoxymethyl)benzene
NINT-008262368-30-9AvailableN-(4-aminophenyl)-2-(4-methylpiperazin-1-yl)acetamide
NINT-024-(Z)-methyl 4-(1,3-dimethoxy-3-oxo-1-phenylprop-1-en-2-yl)-3-nitrobenzoate
NINT-0251644441-68-8Available(Z)-methyl 4-(3-methoxy-1-((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenyl)amino)-3-oxo-1-phenylprop-1-en-2-yl)-3-nitrobenzoate
ProcessRoute 4Steps 2 · Total yield 538 g
Synthetic routes & intermediates Route 4
CodeCAS No.Intermediate
NINT-00414192-26-8Availablemethyl 2-oxo-1,3-dihydroindole-6-carboxylate
NINT-008262368-30-9AvailableN-(4-aminophenyl)-2-(4-methylpiperazin-1-yl)acetamide
NINT-020594-45-6Availableethanesulfonic acid
NINT-02693-58-3Availablemethyl benzoate

Frequently asked questions

What are the approved indications of Nintedanib Esylate?

Approved indications include: Systemic sclerosis-associated interstitial lung disease, Idiopathic pulmonary fibrosis, Non-small cell lung cancer.

When does the Nintedanib Esylate patent expire?

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

How many synthesis routes are recorded for Nintedanib Esylate?

4 synthesis routes are recorded; the shortest is 2 steps with 538 g total yield. Intermediates in each route carry codes and CAS numbers.

Where can I buy Nintedanib Esylate intermediates?

25 intermediate CAS of Nintedanib Esylate 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 Nintedanib Esylate 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