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CAS 136304-78-4

methyl 3-amino-2-(((2'-cyano-[1,1'-biphenyl]-4-yl)methyl)amino)benzoate

Codes: AZILS-002, AZIL-006

Application context (from source-drug indications)

HypertensionAzilsartanEssential hypertensionAzilsartanType 2 diabetesAzilsartanObesityAzilsartanDiabetesAzilsartanHypertensionAzilsartan Medoxomil Potassium/ChlorthalidoneEssential hypertensionAzilsartan Medoxomil Potassium/ChlorthalidoneEssential hypertensionAzilsartan Medoxomil PotassiumHypertensionAzilsartan Medoxomil Potassium

Source drugs (routes using this intermediate)

DrugTierExpiry
AzilsartanTier C — Watch / trade-
Azilsartan Medoxomil Potassium/ChlorthalidoneTier C — Watch / trade-
Azilsartan Medoxomil PotassiumTier C — Watch / trade-

Position in synthesis routes (up/downstream chain)

Ordered by route registration; left → right is the synthesis direction. The highlighted node is the current CAS; others link to their own profiles.

Azilsartan Medoxomil Potassium/ChlorthalidoneOptimised routesteps: 5total yield: 2.9 g
methyl 3-amino-2-(((2'-cyano-[1,1'-biphenyl]-4-yl)methyl)amino)benzoate→methyl 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→2,6-dichloro-9-((3S,4R,5R)-3-fluoro-4-((triisopropylsilyl)oxy)-5-(((triisopropylsilyl)oxy)methyl)tetrahydrofuran-2-yl)-9H-purine→methyl (Z)-3-amino-2-(((2'-(N'-((ethoxycarbonyl)oxy)carbamimidoyl)-[1,1'-biphenyl]-4-yl)methyl)amino)benzoate→methyl (Z)-2-ethoxy-1-((2'-(N'-((ethoxycarbonyl)oxy)carbamimidoyl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate
Azilsartan Medoxomil PotassiumOptimised routesteps: 5total yield: 2.9 g
methyl 3-amino-2-(((2'-cyano-[1,1'-biphenyl]-4-yl)methyl)amino)benzoate→methyl 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→2,6-dichloro-9-((3S,4R,5R)-3-fluoro-4-((triisopropylsilyl)oxy)-5-(((triisopropylsilyl)oxy)methyl)tetrahydrofuran-2-yl)-9H-purine→methyl (Z)-3-amino-2-(((2'-(N'-((ethoxycarbonyl)oxy)carbamimidoyl)-[1,1'-biphenyl]-4-yl)methyl)amino)benzoate→methyl (Z)-2-ethoxy-1-((2'-(N'-((ethoxycarbonyl)oxy)carbamimidoyl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate

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