Unibest 优贝德
← Back to patent-cliff list

利格列汀

Tier C — Watch / trade

Linagliptin · all drugs expiring in 2029 →

Boehringer Ingelheim International Gmbh
Originator
2011
First approval
2029
Expiry (public)
$0.68B ▲
Peak sales
化学药
Type

Targets：DPP4

Brand：欧唐宁、Ondero、Trazenta、Trajenta、Trayenta、Tradjenta

Indications (approved)：二型糖尿病

Regional status

US
批准上市
2011-05-02
EU
批准上市
2011-08-23
China
批准上市
2013-03-26
Japan
批准上市
2011-07-01

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 4 · Total yield /
Synthetic routes & intermediates Route 1
CodeCAS No.Intermediate
LINA-00193703-24-3Available8-bromo-3-methyl-3,7-dihydro-1H-purine-2,6-dione
LINA-0023355-28-0Available1-bromobut-2-yne
LINA-003666816-98-4Available8-bromo-7-(but-2-yn-1-yl)-3-methyl-3,7-dihydro-1H-purine-2,6-dione
LINA-004109113-72-6Available2-(chloromethyl)-4-methylquinazoline
LINA-005853029-57-9Available8-bromo-7-(but-2-yn-1-yl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-3,7-dihydro-1H-purine-2,6-dione
LINA-006309956-78-3Available(R)-tert-butyl piperidin-3-ylcarbamate
LINA-007668273-75-4Availabletert-butyl (R)-(1-(7-(but-2-yn-1-yl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-8-yl)piperidin-3-yl)carbamate
OptimisedRoute 2Steps 3 · Total yield /
Synthetic routes & intermediates Route 2
CodeCAS No.Intermediate
LINA-00193703-24-3Available8-bromo-3-methyl-3,7-dihydro-1H-purine-2,6-dione
LINA-0023355-28-0Available1-bromobut-2-yne
LINA-003666816-98-4Available8-bromo-7-(but-2-yn-1-yl)-3-methyl-3,7-dihydro-1H-purine-2,6-dione
LINA-004109113-72-6Available2-(chloromethyl)-4-methylquinazoline
LINA-005853029-57-9Available8-bromo-7-(but-2-yn-1-yl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-3,7-dihydro-1H-purine-2,6-dione
LINA-008334618-23-4Available(R)-piperidin-3-amine dihydrochloride
OptimisedRoute 3Steps 7 · Total yield /
Synthetic routes & intermediates Route 3
CodeCAS No.Intermediate
LINA-003666816-98-4Available8-bromo-7-(but-2-yn-1-yl)-3-methyl-3,7-dihydro-1H-purine-2,6-dione
LINA-004109113-72-6Available2-(chloromethyl)-4-methylquinazoline
LINA-005853029-57-9Available8-bromo-7-(but-2-yn-1-yl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-3,7-dihydro-1H-purine-2,6-dione
LINA-009551-93-9Available1-(2-aminophenyl)ethan-1-one
LINA-010107-14-2Available2-chloroacetonitrile
LINA-011886588-62-1Available(R)-2-(piperidin-3-yl)isoindoline-1,3-dione (2S,3S)-2,3-dihydroxysuccinate
LINA-012886588-63-2Available(R)-7-(but-2-yn-1-yl)-8-(3-(1,3-dioxoisoindolin-2-yl)piperidin-1-yl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-3,7-dihydro-1H-purine-2,6-dione
LINA-013462-08-8Availablepyridin-3-amine
LINA-01454012-73-6Availablepiperidin-3-amine
LINA-01585-44-9Availableisobenzofuran-1,3-dione
LINA-01662813-09-6Available2-(piperidin-3-yl)isoindoline-1,3-dione
LINA-017147-71-7Available(2S,3S)-2,3-dihydroxysuccinic acid
OptimisedRoute 4Steps 4 · Total yield /
Synthetic routes & intermediates Route 4
CodeCAS No.Intermediate
LINA-005853029-57-9Available8-bromo-7-(but-2-yn-1-yl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-3,7-dihydro-1H-purine-2,6-dione
LINA-01883602-37-3Availableethyl (R)-piperidine-3-carboxylate (2R,3R)-2,3-dihydroxysuccinate
LINA-0191805773-12-9Availableethyl (R)-1-(7-(but-2-yn-1-yl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-8-yl)piperidine-3-carboxylate
LINA-020-(R)-1-(7-(but-2-yn-1-yl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-8-yl)piperidine-3-carboxylic acid
LINA-021(OPr)1770824-68-4Availablepropyl (R)-(1-(7-(but-2-yn-1-yl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-8-yl)piperidin-3-yl)carbamate
LINA-021(C7H5N2S)1383917-89-2Available(R)-N-(1-(7-(but-2-yn-1-yl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-8-yl)piperidin-3-yl)octa-2,4,6-triynamide compound with 1-(l1-sulfanyl)-2l2-diazene and dihydrogen (1:1:1)
LINA-021(S(CH2)11CH3)-S-dodecyl (R)-(1-(7-(but-2-yn-1-yl)-3-methyl-1-((4-methylquinazolin-2-yl)methyl)-2,6-dioxo-2,3,6,7-tetrahydro-1H-purin-8-yl)piperidin-3-yl)carbamothioate

Frequently asked questions

What are the approved indications of Linagliptin?

Approved indications include: 二型糖尿病.

When does the Linagliptin patent expire?

Based on public sources, the Linagliptin patent expires in 2029.

How many synthesis routes are recorded for Linagliptin?

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

Where can I buy Linagliptin intermediates?

21 intermediate CAS of Linagliptin 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 Linagliptin 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