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阿齐沙坦

Tier C — Watch / trade

Azilsartan

武田药品工业株式会社
Originator
2012
First approval
-
Expiry (public)
$0.77B ▲
Peak sales
化学药
Type

Targets：AT1

Brand：Azilva

Indications (approved)：高血压

Regional status

US
终止
2006-06-01
EU
-
China
批准上市
2021-06-18
Japan
批准上市
2012-01-18

Synthetic routes & intermediates6 routes

Originator routes × 1Optimised (non-patent) × 5Process 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 6 · Total yield 0.135 g
Synthetic routes & intermediates Route 1
CodeCAS No.Intermediate
AZILS-001139481-28-0methyl 2-(((2'-cyano-[1,1'-biphenyl]-4-yl)methyl)amino)-3-nitrobenzoate
AZILS-002136304-78-4methyl 3-amino-2-(((2'-cyano-[1,1'-biphenyl]-4-yl)methyl)amino)benzoate
AZILS-00378-09-1triethoxymethoxyethane
AZILS-004139481-44-0methyl 1-((2'-cyano-[1,1'-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate
AZILS-005147403-65-4methyl (Z)-2-ethoxy-1-((2'-(N'-hydroxycarbamimidoyl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate
AZILS-006541-41-3ethyl carbonochloridate
AZILS-007-methyl (Z)-2-ethoxy-1-((2'-(N'-((ethoxycarbonyl)oxy)carbamimidoyl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate
AZILS-008147403-52-9methyl 2-ethoxy-1-((2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate
OptimisedRoute 2Steps 3 · Total yield 173.2 g
Synthetic routes & intermediates Route 2
CodeCAS No.Intermediate
AZILS-008147403-52-9methyl 2-ethoxy-1-((2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate
AZILS-009139481-41-7ethyl 1-((2'-cyano-[1,1'-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate
AZILS-010-2,6-dichloro-9-((3S,4R,5R)-3-fluoro-4-((triisopropylsilyl)oxy)-5-(((triisopropylsilyl)oxy)methyl)tetrahydrofuran-2-yl)-9H-purine
OptimisedRoute 3Steps 5 · Total yield 9.2 g
Synthetic routes & intermediates Route 3
CodeCAS No.Intermediate
AZILS-008147403-52-9methyl 2-ethoxy-1-((2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate
AZILS-011150058-27-8methyl 2-ethoxy-1H-benzo[d]imidazole-7-carboxylate
AZILS-012911314-60-84'-(bromomethyl)-[1,1'-biphenyl]-2-carbaldehyde
AZILS-0131637363-71-3methyl 2-ethoxy-1-((2'-formyl-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate
AZILS-0141637363-72-4methyl (E)-2-ethoxy-1-((2'-((hydroxyimino)methyl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate
AZILS-0151637363-73-5methyl (Z)-1-((2'-(chloro(hydroxyimino)methyl)-[1,1'-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate
OptimisedRoute 4Steps 4 · Total yield 9.5 g
Synthetic routes & intermediates Route 4
CodeCAS No.Intermediate
AZILS-004139481-44-0methyl 1-((2'-cyano-[1,1'-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate
AZILS-008147403-52-9methyl 2-ethoxy-1-((2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate
AZILS-011150058-27-8methyl 2-ethoxy-1H-benzo[d]imidazole-7-carboxylate
AZILS-016107582-20-7methyl 2,3-diaminobenzoate
AZILS-017114772-54-24'-(bromomethyl)-[1,1'-biphenyl]-2-carbonitrile
OptimisedRoute 5Steps 2 · Total yield 7.5 g
Synthetic routes & intermediates Route 5
CodeCAS No.Intermediate
AZILS-004139481-44-0methyl 1-((2'-cyano-[1,1'-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate
AZILS-005-2,6-dichloro-9-((3S,4R,5R)-3-fluoro-4-((triisopropylsilyl)oxy)-5-(((triisopropylsilyl)oxy)methyl)tetrahydrofuran-2-yl)-9H-purine
OptimisedRoute 6Steps 5 · Total yield 13.5 g
Synthetic routes & intermediates Route 6
CodeCAS No.Intermediate
AZILS-018114772-53-14'-methyl-[1,1'-biphenyl]-2-carbonitrile
AZILS-019-2,6-dichloro-9-((3S,4R,5R)-3-fluoro-4-((triisopropylsilyl)oxy)-5-(((triisopropylsilyl)oxy)methyl)tetrahydrofuran-2-yl)-9H-purine
AZILS-020161862-33-53-(4'-methyl-[1,1'-biphenyl]-2-yl)-1,2,4-oxadiazol-5(4H)-one
AZILS-021161862-32-43-(4'-(bromomethyl)-[1,1'-biphenyl]-2-yl)-1,2,4-oxadiazol-5(4H)-one
AZILS-022d-2,6-dichloro-9-((3S,4R,5R)-3-fluoro-4-((triisopropylsilyl)oxy)-5-(((triisopropylsilyl)oxy)methyl)tetrahydrofuran-2-yl)-9H-purine
AZILS-022b577957-02-9ethyl 2-ethoxy-1H-benzo[d]imidazole-7-carboxylate
AZILS-022a150058-27-8methyl 2-ethoxy-1H-benzo[d]imidazole-7-carboxylate
AZILS-022c-2,6-dichloro-9-((3S,4R,5R)-3-fluoro-4-((triisopropylsilyl)oxy)-5-(((triisopropylsilyl)oxy)methyl)tetrahydrofuran-2-yl)-9H-purine
AZILS-023c-2,6-dichloro-9-((3S,4R,5R)-3-fluoro-4-((triisopropylsilyl)oxy)-5-(((triisopropylsilyl)oxy)methyl)tetrahydrofuran-2-yl)-9H-purine
AZILS-023b1403474-70-3ethyl 2-ethoxy-1-((2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate
AZILS-023a147403-52-9methyl 2-ethoxy-1-((2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate
AZILS-023d-2,6-dichloro-9-((3S,4R,5R)-3-fluoro-4-((triisopropylsilyl)oxy)-5-(((triisopropylsilyl)oxy)methyl)tetrahydrofuran-2-yl)-9H-purine

Frequently asked questions

What are the approved indications of Azilsartan?

Approved indications include: 高血压.

When does the Azilsartan patent expire?

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

How many synthesis routes are recorded for Azilsartan?

6 synthesis routes are recorded; the shortest is 2 steps with 7.5 g total yield. Intermediates in each route carry codes and CAS numbers.

Where can I buy Azilsartan intermediates?

All intermediates in Azilsartan routes have CAS profiles — you can submit an RFQ per CAS and it enters the Unibest matching pool.

How do I get a quote for Azilsartan 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