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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 720698Generated: October 28, 2026

4-[(4-(Hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-alpha,alpha-dimethylbenzeneacetic acid hydrochloride hydrate → Fexofenadine Hydrochloride

https://huagongshe.com/reaction/720698

Reaction equation

Participants

RoleNameHCIDCharge
Reactant4-[(4-(Hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-alpha,alpha-dimethylbenzeneacetic acid hydrochloride hydrateHCID 11613748—
SolventMethyl Ethyl KetoneHCID 6569—
ProductFexofenadine HydrochlorideHCID 6300297%

Reaction Conditions

Temperature-15 °C

Reaction Steps

Treat 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-α,α-dimethylbenzeneacetic acid hydrochloride hydrate (Form II) (5.00 g, 0.0083 mol) with methylethyl ketone (130 mL). Slowly add water (0.4 mL), filter through filter aid and wash the filter cake with methylethyl ketone (20 mL). Heat to reflux and distill off 75 mL of solvent, cool to −15° C. and collect by vacuum filtration. Wash with methylethyl ketone (2×10 mL) and vacuum dry at 60° C. to give the title compound (4.33 g, 97%); mp 196–198° C.

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS07135571B2
Source datasetuspto-grants-2006_11
ORD IDord-a988a3de31d4411ea6ad1db78958c60b
Source noteuspto-grants-2006_11