1-((4-Chlorphenyl)phenylmethyl)-4-((4-(1,1-dimethylethyl)phenyl)-methyl)piperazin-dihydrochlorid

BUCLIZINE, DIHYDROCHLORIDE Chemische Eigenschaften,Einsatz,Produktion Methoden

• Chemische Eigenschaften

  BUCLIZINE, DIHYDROCHLORIDE is Off-White Powder

• Originator

  Longifine,UCB

• Verwenden

  BUCLIZINE, DIHYDROCHLORIDE used as an antiemetic

• Definition

  ChEBI: Buclizine dihydrochloride is a hydrochloride salt that is obtained by reaction of buclizine with 2 equivalents of hydrogen chloride. It has a role as a central nervous system depressant, a local anaesthetic, a histamine antagonist, a cholinergic antagonist and an antiemetic. It contains a buclizine(2+).

• Manufacturing Process

  1 mol 4-chlorobenzhydril chloride was heated in toluene to reflux with 1 mol ethyl ester of piperazine 1-carboxylic acid at about 150°C in a presence of an excess of triethyl amine. On cooling the triethyl amine hydrochloride was filtered off, a solvent was removed in vacuum and the residue [(4-chlorophenyl)- phenyl-methyl]piperazine carboxylic acid ethyl ester was boiled straight away with potassium hydroxide in ethanol for 48 hours. After removing ethanol in vacuum to dryness, the residue was dissolved in benzene and washed with water. The benzene solution was dried, benzene removed in vacuum. The residue was distilled to give 4-chlorobezhydryl-piperazine. It had given the desired 1-(p-tert-butylbenzyl)-4-(p-chloro-α-phenylbenzyl)- piperazine, buclizine, by a reaction with 4-tert-butylbenzyl chloride in the presence of any halogen hydrochloride acceptor (triethyl amine, sodium or potassium carbonate and so on). The obtained product had BP: 230°- 240°C/0.001 mm Hg.

• Trademarks

  Bucladin (Stuart).

• Therapeutic Function

  Antihistaminic, Antiallergic, Antinauseant, Tranquilizer, Appetite stimulant

• Allgemeine Beschreibung

  Buclizine hydrochloride, l-(p-tertbutylbenzyl)-4-(p-chloro-α-phenylbenzyl)piperazinedihydrochloride (Bucladin-S), is a white to slightly yellowcrystalline powder that is insoluble in water. The highlylipid-soluble buclizine has CNS depressant, antiemetic, andantihistaminic properties. This drug has been discontinued inthe United States.

• Biologische Aktivität

  Buclizine is a piperazine antihistamine and anticholinergic th at exerts its antiemetic and antimotion sickness effects.', 'Histamine H1 receptor antagonist

• Sicherheitsprofil

  Poison by intraperitoneal route. An experimental teratogen. When heated to decomposition it emits very toxic fumes of NOx, and HCl.

BUCLIZINE, DIHYDROCHLORIDE Upstream-Materialien And Downstream Produkte

1-((4-Chlorphenyl)phenylmethyl)-4-((4-(1,1-dimethylethyl)phenyl)-methyl)piperazin-dihydrochlorid Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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