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CAS 124750-51-2
5-(4'-(bromomethyl)-[1,1'-biphenyl]-2-yl)-1-trityl-1H-tetrazole
Codes: FIMA-004, OLME-006, CAND-026
Application context (from source-drug indications)
Essential hypertensionAmlodipine Besylate/Fimasartan PotassiumHypertensionAmlodipine Besylate/Fimasartan PotassiumHypertensionOlmesartan Medoxomil/Amlodipine MaleateHypertensionOlmesartan Medoxomil/Amlodipine orotateHypertensionAmlodipine Besylate/Candesartan CilexetilHypertensionOlmesartan Medoxomil/AzelnidipineEssential hypertensionAmlodipine Besylate/Olmesartan MedoxomilHypertensionAmlodipine Besylate/Olmesartan MedoxomilHypertensionOlmesartan MedoxomilIschaemic strokeOlmesartan MedoxomilHeart failureOlmesartan MedoxomilMetabolic syndromeOlmesartan MedoxomilGlomerulonephritisOlmesartan MedoxomilType 2 diabetesOlmesartan MedoxomilHypertensionFimasartan Potassium TrihydrateEssential hypertensionFimasartan Potassium TrihydrateHypercholesterolaemiaFimasartan Potassium TrihydrateChronic renal impairmentFimasartan Potassium TrihydrateRenal impairmentFimasartan Potassium TrihydrateHepatic function declineFimasartan Potassium TrihydrateHypertensionCandesartan CilexetilHeart failureCandesartan CilexetilEssential hypertensionCandesartan CilexetilMigraineCandesartan CilexetilCOVID-19Candesartan CilexetilManiaCandesartan Cilexetil
Source drugs (routes using this intermediate)
| Drug | Tier | Expiry |
|---|---|---|
| Amlodipine Besylate/Fimasartan Potassium | Tier C — Watch / trade | - |
| Olmesartan Medoxomil/Amlodipine Maleate | Tier C — Watch / trade | - |
| Olmesartan Medoxomil/Amlodipine orotate | Tier C — Watch / trade | - |
| Amlodipine Besylate/Candesartan Cilexetil | Tier C — Watch / trade | - |
| Olmesartan Medoxomil/Azelnidipine | Tier C — Watch / trade | - |
| Amlodipine Besylate/Olmesartan Medoxomil | Tier C — Watch / trade | - |
| Olmesartan Medoxomil | Tier B — Position early | - |
| Fimasartan Potassium Trihydrate | Tier C — Watch / trade | - |
| Candesartan Cilexetil | Tier B — Position early | - |
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.
diethyl 2-acetylsuccinate→pentanimidamide→ethyl 2-(2-butyl-4-methyl-6-oxo-1,6-dihydropyrimidin-5-yl)acetate→5-(4'-(bromomethyl)-[1,1'-biphenyl]-2-yl)-1-trityl-1H-tetrazole→ethyl 2-(2-butyl-4-methyl-6-oxo-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1,6-dihydropyrimidin-5-yl)acetate→ethyl 2-(2-butyl-4-methyl-6-oxo-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1,6-dihydropyrimidin-5-yl)acetate→2-(2-butyl-4-methyl-6-oxo-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1,6-dihydropyrimidin-5-yl)-N,N-dimethylacetamide→2-(2-butyl-4-methyl-6-oxo-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1,6-dihydropyrimidin-5-yl)acetic acid
5-(4'-(bromomethyl)-[1,1'-biphenyl]-2-yl)-1-trityl-1H-tetrazole→2-(2-butyl-4-methyl-6-oxo-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1,6-dihydropyrimidin-5-yl)-N,N-dimethylacetamide→methyl 3-oxobutanoate→2-chloro-N,N-dimethylacetamide→methyl 2-acetyl-4-(dimethylamino)-4-oxobutanoate→ pentanimidamide;hydrochloride→methyl 2-acetyl-4-(dimethylamino)-4-oxobutanoate
5-(4'-(bromomethyl)-[1,1'-biphenyl]-2-yl)-1-trityl-1H-tetrazole→4'-methyl-[1,1'-biphenyl]-2-carbonitrile→5-(4'-methyl-[1,1'-biphenyl]-2-yl)-1H-tetrazole→5-(4'-methyl-[1,1'-biphenyl]-2-yl)-1-trityl-1H-tetrazole
(2R,3R,4R,5S)-2-((benzoyloxy)methyl)-5-bromotetrahydrofuran-3,4-diyl dibenzoate→1,1,1-trimethoxybutane→2-propyl-1H-imidazole-4,5-dicarbonitrile→diethyl 2-propyl-1H-imidazole-4,5-dicarboxylate→ethyl 4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylate→5-(4'-(bromomethyl)-[1,1'-biphenyl]-2-yl)-1-trityl-1H-tetrazole→ethyl 4-(2-hydroxypropan-2-yl)-2-propyl-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-imidazole-5-carboxylate→lithium 4-(2-hydroxypropan-2-yl)-2-propyl-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-imidazole-5-carboxylate→4-(chloromethyl)-5-methyl-1,3-dioxol-2-one→(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 4-(2-hydroxypropan-2-yl)-2-propyl-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-imidazole-5-carboxylate
ethyl 4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylate→5-(4'-(bromomethyl)-[1,1'-biphenyl]-2-yl)-1-trityl-1H-tetrazole→4-(chloromethyl)-5-methyl-1,3-dioxol-2-one→(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 4-(2-hydroxypropan-2-yl)-2-propyl-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-imidazole-5-carboxylate→4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylic acid→(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylate
(2R,3R,4R,5S)-2-((benzoyloxy)methyl)-5-bromotetrahydrofuran-3,4-diyl dibenzoate→1,1,1-trimethoxybutane→2-propyl-1H-imidazole-4,5-dicarbonitrile→diethyl 2-propyl-1H-imidazole-4,5-dicarboxylate→ethyl 4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylate→5-(4'-(bromomethyl)-[1,1'-biphenyl]-2-yl)-1-trityl-1H-tetrazole→ethyl 4-(2-hydroxypropan-2-yl)-2-propyl-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-imidazole-5-carboxylate→lithium 4-(2-hydroxypropan-2-yl)-2-propyl-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-imidazole-5-carboxylate→4-(chloromethyl)-5-methyl-1,3-dioxol-2-one→(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 4-(2-hydroxypropan-2-yl)-2-propyl-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-imidazole-5-carboxylate
ethyl 4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylate→5-(4'-(bromomethyl)-[1,1'-biphenyl]-2-yl)-1-trityl-1H-tetrazole→4-(chloromethyl)-5-methyl-1,3-dioxol-2-one→(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 4-(2-hydroxypropan-2-yl)-2-propyl-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-imidazole-5-carboxylate→4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylic acid→(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylate
1-chloroethyl cyclohexyl carbonate→1-(((cyclohexyloxy)carbonyl)oxy)ethyl 2-ethoxy-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate→2-nitrobenzoic acid→methyl 2-nitrobenzoate→methyl 2-aminobenzoate→methyl 2-((ethoxycarbonyl)amino)-3-nitrobenzoate→5-(4'-(bromomethyl)-[1,1'-biphenyl]-2-yl)-1-trityl-1H-tetrazole→methyl 2-((ethoxycarbonyl)((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)amino)-3-nitrobenzoate→methyl 3-amino-2-((ethoxycarbonyl)((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)amino)benzoate→methyl 2-ethoxy-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate
(2R,3R,4R,5S)-2-((benzoyloxy)methyl)-5-bromotetrahydrofuran-3,4-diyl dibenzoate→1,1,1-trimethoxybutane→2-propyl-1H-imidazole-4,5-dicarbonitrile→diethyl 2-propyl-1H-imidazole-4,5-dicarboxylate→ethyl 4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylate→5-(4'-(bromomethyl)-[1,1'-biphenyl]-2-yl)-1-trityl-1H-tetrazole→ethyl 4-(2-hydroxypropan-2-yl)-2-propyl-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-imidazole-5-carboxylate→lithium 4-(2-hydroxypropan-2-yl)-2-propyl-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-imidazole-5-carboxylate→4-(chloromethyl)-5-methyl-1,3-dioxol-2-one→(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 4-(2-hydroxypropan-2-yl)-2-propyl-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-imidazole-5-carboxylate
ethyl 4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylate→5-(4'-(bromomethyl)-[1,1'-biphenyl]-2-yl)-1-trityl-1H-tetrazole→4-(chloromethyl)-5-methyl-1,3-dioxol-2-one→(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 4-(2-hydroxypropan-2-yl)-2-propyl-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-imidazole-5-carboxylate→4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylic acid→(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylate
(2R,3R,4R,5S)-2-((benzoyloxy)methyl)-5-bromotetrahydrofuran-3,4-diyl dibenzoate→1,1,1-trimethoxybutane→2-propyl-1H-imidazole-4,5-dicarbonitrile→diethyl 2-propyl-1H-imidazole-4,5-dicarboxylate→ethyl 4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylate→5-(4'-(bromomethyl)-[1,1'-biphenyl]-2-yl)-1-trityl-1H-tetrazole→ethyl 4-(2-hydroxypropan-2-yl)-2-propyl-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-imidazole-5-carboxylate→lithium 4-(2-hydroxypropan-2-yl)-2-propyl-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-imidazole-5-carboxylate→4-(chloromethyl)-5-methyl-1,3-dioxol-2-one→(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 4-(2-hydroxypropan-2-yl)-2-propyl-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-imidazole-5-carboxylate
ethyl 4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylate→5-(4'-(bromomethyl)-[1,1'-biphenyl]-2-yl)-1-trityl-1H-tetrazole→4-(chloromethyl)-5-methyl-1,3-dioxol-2-one→(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 4-(2-hydroxypropan-2-yl)-2-propyl-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-imidazole-5-carboxylate→4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylic acid→(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylate
(2R,3R,4R,5S)-2-((benzoyloxy)methyl)-5-bromotetrahydrofuran-3,4-diyl dibenzoate→1,1,1-trimethoxybutane→2-propyl-1H-imidazole-4,5-dicarbonitrile→diethyl 2-propyl-1H-imidazole-4,5-dicarboxylate→ethyl 4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylate→5-(4'-(bromomethyl)-[1,1'-biphenyl]-2-yl)-1-trityl-1H-tetrazole→ethyl 4-(2-hydroxypropan-2-yl)-2-propyl-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-imidazole-5-carboxylate→lithium 4-(2-hydroxypropan-2-yl)-2-propyl-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-imidazole-5-carboxylate→4-(chloromethyl)-5-methyl-1,3-dioxol-2-one→(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 4-(2-hydroxypropan-2-yl)-2-propyl-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-imidazole-5-carboxylate
ethyl 4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylate→5-(4'-(bromomethyl)-[1,1'-biphenyl]-2-yl)-1-trityl-1H-tetrazole→4-(chloromethyl)-5-methyl-1,3-dioxol-2-one→(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 4-(2-hydroxypropan-2-yl)-2-propyl-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-imidazole-5-carboxylate→4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylic acid→(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylate
diethyl 2-acetylsuccinate→pentanimidamide→ethyl 2-(2-butyl-4-methyl-6-oxo-1,6-dihydropyrimidin-5-yl)acetate→5-(4'-(bromomethyl)-[1,1'-biphenyl]-2-yl)-1-trityl-1H-tetrazole→ethyl 2-(2-butyl-4-methyl-6-oxo-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1,6-dihydropyrimidin-5-yl)acetate→ethyl 2-(2-butyl-4-methyl-6-oxo-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1,6-dihydropyrimidin-5-yl)acetate→2-(2-butyl-4-methyl-6-oxo-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1,6-dihydropyrimidin-5-yl)-N,N-dimethylacetamide→2-(2-butyl-4-methyl-6-oxo-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1,6-dihydropyrimidin-5-yl)acetic acid
5-(4'-(bromomethyl)-[1,1'-biphenyl]-2-yl)-1-trityl-1H-tetrazole→2-(2-butyl-4-methyl-6-oxo-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1,6-dihydropyrimidin-5-yl)-N,N-dimethylacetamide→methyl 3-oxobutanoate→2-chloro-N,N-dimethylacetamide→methyl 2-acetyl-4-(dimethylamino)-4-oxobutanoate→ pentanimidamide;hydrochloride→methyl 2-acetyl-4-(dimethylamino)-4-oxobutanoate
5-(4'-(bromomethyl)-[1,1'-biphenyl]-2-yl)-1-trityl-1H-tetrazole→4'-methyl-[1,1'-biphenyl]-2-carbonitrile→5-(4'-methyl-[1,1'-biphenyl]-2-yl)-1H-tetrazole→5-(4'-methyl-[1,1'-biphenyl]-2-yl)-1-trityl-1H-tetrazole
1-chloroethyl cyclohexyl carbonate→1-(((cyclohexyloxy)carbonyl)oxy)ethyl 2-ethoxy-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate→2-nitrobenzoic acid→methyl 2-nitrobenzoate→methyl 2-aminobenzoate→methyl 2-((ethoxycarbonyl)amino)-3-nitrobenzoate→5-(4'-(bromomethyl)-[1,1'-biphenyl]-2-yl)-1-trityl-1H-tetrazole→methyl 2-((ethoxycarbonyl)((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)amino)-3-nitrobenzoate→methyl 3-amino-2-((ethoxycarbonyl)((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)amino)benzoate→methyl 2-ethoxy-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate
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