CAS 115-46-8

methanol

Codes: FEXO-006

Application context (from source-drug indications)

Allergic rhinitisFexofenadine HydrochlorideDermatitisFexofenadine HydrochloridePruritusFexofenadine HydrochlorideEczemaFexofenadine HydrochlorideAtopic dermatitisFexofenadine HydrochlorideSeasonal allergic rhinitisFexofenadine Hydrochloride

Source drugs (routes using this intermediate)

Drug	Tier	Expiry
Fexofenadine Hydrochloride	Tier 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.

Fexofenadine HydrochlorideOriginator routesteps: 7total yield: /

2-methyl-2-phenylpropanoic acid→2-methyl-2-phenylpropan-1-ol→2-methyl-2-phenylpropyl acetate→4-chlorobutanoyl chloride→2-(4-(4-chlorobutanoyl)phenyl)-2-methylpropyl acetate→methanol→2-(4-(4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butanoyl)phenyl)-2-methylpropyl acetate→1-(4-(1-hydroxy-2-methylpropan-2-yl)phenyl)-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butan-1-one→2-(4-(4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butanoyl)phenyl)-2-methylpropanoic acid

Fexofenadine HydrochlorideOptimised routesteps: 4total yield: /

methanol→ethyl 2-(4-formylphenyl)-2-methylpropanoate→(2-(1,3-dioxolan-2-yl)ethyl)magnesium bromide→ethyl 2-(4-(3-(1,3-dioxolan-2-yl)-1-hydroxypropyl)phenyl)-2-methylpropanoate→ethyl 2-(4-(5-hydroxytetrahydrofuran-2-yl)phenyl)-2-methylpropanoate→ethyl 2-(4-(1-hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoate

Fexofenadine HydrochlorideOptimised routesteps: 5total yield: 3.30 g

methanol→methyl 2-methyl-2-phenylpropanoate→dihydrofuran-2,5-dione→4-(4-(1-methoxy-2-methyl-1-oxopropan-2-yl)phenyl)-4-oxobutanoic acid→2-phenylethanamine→2-phenylethanamine 4-(4-(1-methoxy-2-methyl-1-oxopropan-2-yl)phenyl)-4-oxobutanoate→methyl 2-(4-(4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)-4-oxobutanoyl)phenyl)-2-methylpropanoate→methyl 2-(4-(1-hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoate

Fexofenadine HydrochlorideOptimised routesteps: 4total yield: 6.70 g

methanol→ethyl 2-(4-(5-hydroxytetrahydrofuran-2-yl)phenyl)-2-methylpropanoate→methyl 2-(4-(4-hydroxybut-1-yn-1-yl)phenyl)-2-methylpropanoate→methyl 2-(4-(4-bromobutanoyl)phenyl)-2-methylpropanoate→methyl 2-(4-(4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butanoyl)phenyl)-2-methylpropanoate

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