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CAS 459-57-4

4-fluorobenzaldehyde(4-Fluorophenyl)methanone4-Fluorobenzaldehyde

Codes: PIMAV-014, Tamsulosin Hydrochloride-023, ROSU-001, LOBE-006, ESCI-021, Mosapride Citrate-017

Application context (from source-drug indications)

DelusionPimavanserin TartrateHallucinationPimavanserin TartrateErectile dysfunctionTadalafil/TamsulosinBenign prostatic hyperplasiaTadalafil/TamsulosinHypertensionFimasartan potassium trihydrate/Rosuvastatin calciumDyslipidaemiaFimasartan potassium trihydrate/Rosuvastatin calciumHypertensionRosuvastatin Calcium/TelmisartanHyperlipidaemiaRosuvastatin Calcium/TelmisartanLower urinary tract symptomsSolifenacin Succinate/Tamsulosin HydrochlorideBenign prostatic hyperplasiaSolifenacin Succinate/Tamsulosin HydrochlorideOveractive bladderSolifenacin Succinate/Tamsulosin HydrochlorideDrug-related adverse effects and reactionsSolifenacin Succinate/Tamsulosin HydrochlorideBladder neck obstructionSolifenacin Succinate/Tamsulosin HydrochlorideType 2 diabetesLobeglitazone SulfateGastroparesisLobeglitazone SulfateRenal impairmentLobeglitazone SulfateAbnormal liver functionLobeglitazone SulfateBenign prostatic hyperplasiaDutasteride/Tamsulosin HydrochlorideBenign prostatic hyperplasiaTamsulosin HydrochlorideUrinary tract infectionTamsulosin HydrochlorideUrinary retentionTamsulosin HydrochlorideInguinal herniaTamsulosin HydrochlorideVoiding dysfunctionTamsulosin HydrochlorideLower urinary tract symptomsTamsulosin HydrochlorideHomozygous familial hypercholesterolaemiaRosuvastatin CalciumHeterozygous familial hypercholesterolaemiaRosuvastatin CalciumHyperlipoproteinaemia type IIIRosuvastatin CalciumAtherosclerosisRosuvastatin CalciumHyperlipoproteinaemia type IIRosuvastatin CalciumHypercholesterolaemiaRosuvastatin Calcium社交恐惧症Escitalopram OxalateMajor depressive disorderEscitalopram OxalatePanic disorderEscitalopram OxalateDepressionEscitalopram OxalateAnxiety disorderEscitalopram OxalateIrritable bowel syndromeEscitalopram OxalateGastritisMosapride CitrateEnteral feeding intoleranceMosapride CitrateIrritable bowel syndromeMosapride CitrateDyspepsiaMosapride CitrateConstipationMosapride Citrate

Source drugs (routes using this intermediate)

DrugTierExpiry
Pimavanserin TartrateTier C — Watch / trade2029
Tadalafil/TamsulosinTier C — Watch / trade-
Fimasartan potassium trihydrate/Rosuvastatin calciumTier C — Watch / trade-
Rosuvastatin Calcium/TelmisartanTier C — Watch / trade-
Solifenacin Succinate/Tamsulosin HydrochlorideTier C — Watch / trade-
Lobeglitazone SulfateTier C — Watch / trade-
Dutasteride/Tamsulosin HydrochlorideTier C — Watch / trade-
Tamsulosin HydrochlorideTier C — Watch / trade-
Rosuvastatin CalciumTier B — Position early-
Escitalopram OxalateTier B — Position early-
Mosapride CitrateTier 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.

Tadalafil/TamsulosinOptimised routesteps: 4total yield: 18g(Tamsulosin Hydrochloride (API))
5-(2(R)-Aminopropyl)-2-methoxybenzenesulfonamide→Benzaldehyde→4-Methoxybenzaldehyde→4-Formylphenol→(4-Fluorophenyl)methanone→2-methoxy-5-[(2R)-2-[(E)-(phenylmethylidene)amino]propyl]benzene-1-sulfonamide→2-Methoxy-5-[(2R)-2-[(E)-[(4-methoxyphenyl)methylidene]amino]propyl]benzene-1-sulfonamide→5-[(2R)-2-[(E)-[(4-Hydroxyphenyl)methylidene]amino]propyl]-2-methoxybenzene-1-sulfonamide→5-[(2R)-2-[(E)-[(4-Fluorophenyl)methylidene]amino]propyl]-2-methoxybenzene-1-sulfonamide→1-ethoxy-2-(2-iodoethoxy)benzene→(E)-[2-(2-ethoxyphenoxy)ethyl][(2R)-1-(4-methoxy-3-sulfamoylphenyl)propan-2-yl](phenylmethylidene)azanium iodide→(2R)-N-[2-(2-Ethoxyphenoxy)ethyl]-N-[(E)-(4-methoxyphenyl)methylidene]-1-(4-methoxy-3-sulfamoylphenyl)propan-2-iminium iodide→(2R)-N-[2-(2-Ethoxyphenoxy)ethyl]-N-[(E)-(4-hydroxyphenyl)methylidene]-1-(4-methoxy-3-sulfamoylphenyl)propan-2-iminium iodide→(2R)-N-[2-(2-Ethoxyphenoxy)ethyl]-N-[(E)-(4-fluorophenyl)methylidene]-1-(4-methoxy-3-sulfamoylphenyl)propan-2-iminium iodide→(-)-5-[2(R)-[2-(2-Ethoxyphenoxy)ethylamino]propyl]-2-methoxybenzenesulfonamide
Solifenacin Succinate/Tamsulosin HydrochlorideOptimised routesteps: 4total yield: 18g(Tamsulosin Hydrochloride (API))
5-(2(R)-Aminopropyl)-2-methoxybenzenesulfonamide→Benzaldehyde→4-Methoxybenzaldehyde→4-Formylphenol→(4-Fluorophenyl)methanone→2-methoxy-5-[(2R)-2-[(E)-(phenylmethylidene)amino]propyl]benzene-1-sulfonamide→2-Methoxy-5-[(2R)-2-[(E)-[(4-methoxyphenyl)methylidene]amino]propyl]benzene-1-sulfonamide→5-[(2R)-2-[(E)-[(4-Hydroxyphenyl)methylidene]amino]propyl]-2-methoxybenzene-1-sulfonamide→5-[(2R)-2-[(E)-[(4-Fluorophenyl)methylidene]amino]propyl]-2-methoxybenzene-1-sulfonamide→1-ethoxy-2-(2-iodoethoxy)benzene→(E)-[2-(2-ethoxyphenoxy)ethyl][(2R)-1-(4-methoxy-3-sulfamoylphenyl)propan-2-yl](phenylmethylidene)azanium iodide→(2R)-N-[2-(2-Ethoxyphenoxy)ethyl]-N-[(E)-(4-methoxyphenyl)methylidene]-1-(4-methoxy-3-sulfamoylphenyl)propan-2-iminium iodide→(2R)-N-[2-(2-Ethoxyphenoxy)ethyl]-N-[(E)-(4-hydroxyphenyl)methylidene]-1-(4-methoxy-3-sulfamoylphenyl)propan-2-iminium iodide→(2R)-N-[2-(2-Ethoxyphenoxy)ethyl]-N-[(E)-(4-fluorophenyl)methylidene]-1-(4-methoxy-3-sulfamoylphenyl)propan-2-iminium iodide→(-)-5-[2(R)-[2-(2-Ethoxyphenoxy)ethylamino]propyl]-2-methoxybenzenesulfonamide
Dutasteride/Tamsulosin HydrochlorideOptimised routesteps: 4total yield: 18g(Tamsulosin Hydrochloride (API))
5-(2(R)-Aminopropyl)-2-methoxybenzenesulfonamide→Benzaldehyde→4-Methoxybenzaldehyde→4-Formylphenol→(4-Fluorophenyl)methanone→2-methoxy-5-[(2R)-2-[(E)-(phenylmethylidene)amino]propyl]benzene-1-sulfonamide→2-Methoxy-5-[(2R)-2-[(E)-[(4-methoxyphenyl)methylidene]amino]propyl]benzene-1-sulfonamide→5-[(2R)-2-[(E)-[(4-Hydroxyphenyl)methylidene]amino]propyl]-2-methoxybenzene-1-sulfonamide→5-[(2R)-2-[(E)-[(4-Fluorophenyl)methylidene]amino]propyl]-2-methoxybenzene-1-sulfonamide→1-ethoxy-2-(2-iodoethoxy)benzene→(E)-[2-(2-ethoxyphenoxy)ethyl][(2R)-1-(4-methoxy-3-sulfamoylphenyl)propan-2-yl](phenylmethylidene)azanium iodide→(2R)-N-[2-(2-Ethoxyphenoxy)ethyl]-N-[(E)-(4-methoxyphenyl)methylidene]-1-(4-methoxy-3-sulfamoylphenyl)propan-2-iminium iodide→(2R)-N-[2-(2-Ethoxyphenoxy)ethyl]-N-[(E)-(4-hydroxyphenyl)methylidene]-1-(4-methoxy-3-sulfamoylphenyl)propan-2-iminium iodide→(2R)-N-[2-(2-Ethoxyphenoxy)ethyl]-N-[(E)-(4-fluorophenyl)methylidene]-1-(4-methoxy-3-sulfamoylphenyl)propan-2-iminium iodide→(-)-5-[2(R)-[2-(2-Ethoxyphenoxy)ethylamino]propyl]-2-methoxybenzenesulfonamide
Tamsulosin HydrochlorideOptimised routesteps: 4total yield: 18g(Tamsulosin Hydrochloride (API))
5-(2(R)-Aminopropyl)-2-methoxybenzenesulfonamide→Benzaldehyde→4-Methoxybenzaldehyde→4-Formylphenol→(4-Fluorophenyl)methanone→2-methoxy-5-[(2R)-2-[(E)-(phenylmethylidene)amino]propyl]benzene-1-sulfonamide→2-Methoxy-5-[(2R)-2-[(E)-[(4-methoxyphenyl)methylidene]amino]propyl]benzene-1-sulfonamide→5-[(2R)-2-[(E)-[(4-Hydroxyphenyl)methylidene]amino]propyl]-2-methoxybenzene-1-sulfonamide→5-[(2R)-2-[(E)-[(4-Fluorophenyl)methylidene]amino]propyl]-2-methoxybenzene-1-sulfonamide→1-ethoxy-2-(2-iodoethoxy)benzene→(E)-[2-(2-ethoxyphenoxy)ethyl][(2R)-1-(4-methoxy-3-sulfamoylphenyl)propan-2-yl](phenylmethylidene)azanium iodide→(2R)-N-[2-(2-Ethoxyphenoxy)ethyl]-N-[(E)-(4-methoxyphenyl)methylidene]-1-(4-methoxy-3-sulfamoylphenyl)propan-2-iminium iodide→(2R)-N-[2-(2-Ethoxyphenoxy)ethyl]-N-[(E)-(4-hydroxyphenyl)methylidene]-1-(4-methoxy-3-sulfamoylphenyl)propan-2-iminium iodide→(2R)-N-[2-(2-Ethoxyphenoxy)ethyl]-N-[(E)-(4-fluorophenyl)methylidene]-1-(4-methoxy-3-sulfamoylphenyl)propan-2-iminium iodide→(-)-5-[2(R)-[2-(2-Ethoxyphenoxy)ethylamino]propyl]-2-methoxybenzenesulfonamide
Mosapride CitrateOptimised routesteps: 6total yield: /

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