CLEMASTINE FUMARATE

Bezeichnung:CLEMASTINE FUMARATE

CAS-Nr15686-51-8

Englisch Name:CLEMASTINE FUMARATE

CBNumberCB3376056

SummenformelC21H26ClNO

Molgewicht343.89

MOL-Datei15686-51-8.mol

CLEMASTINE FUMARATE physikalisch-chemischer Eigenschaften

alpha	D20 +33.6° (ethanol)
Siedepunkt	bp0.02 154°
Dichte	1.097±0.06 g/cm3(Predicted)
Brechungsindex	nD22 1.5582
Aggregatzustand	Solid
pka	10.23±0.40(Predicted)
Farbe	White to off-white
CAS Datenbank	15686-51-8(CAS DataBase Reference)

CLEMASTINE FUMARATE Chemische Eigenschaften,Einsatz,Produktion Methoden

Originator
Tavegyl,Sandoz,France,1967
Verwenden
Clemastine is used for allergy symptoms, rhinites, Quinke’s edema, anaphylactic shock, hay fever, allergic dermatitis and dermatosis, and chronic eczema. Synonyms of this drug are tavegil and meclastine.
Verwenden
Antihistaminic.
Definition
ChEBI: 2-[(2R)-1-Methylpyrrolidin-2-yl]ethanol in which the hydrogen of the hydroxy group is substituted by a 1-(4-chlorophenyl)-1-phenylethyl group (R configuration). An antihistamine with antimuscarinic and moderate sedative pr perties, it is used as its fumarate salt for the symptomatic relief of allergic conditions such as rhinitis, urticaria, conjunctivitis and in pruritic (severe itching) skin conditions.
Manufacturing Process
9.9 g of α-methyl-p-chlorobenzhydrol are added to a suspension of 2.3 g of powdered sodamide in 30 cc of benzene. Subsequently 7.4 g of Nmethylpyrrolidyl-(2)-ethyl chloride are added and the solution is heated to the boil at reflux for 20 hours. Then shaking is first effected with water and then 4 times each time with 25 cc of 2 N hydrochloric acid. The acid extracts are made alkaline with potassium hydroxide solution while cooling strongly, and the precipitated oil is extracted with ether. After drying of the ethereal solution over potassium carbonate, the solvent is evaporated and the residue is fractionally distilled in a high vacuum, whereby N-methyl-2-[2'-(α-methyl-pchlorobenzhydryloxy)-ethyl]-pyrrolidine boils over at 154°C/0.02 mm Hg. The base is converted to the fumarate by reaction with fumaric acid.
Trademarks
Tavist (Novartis);Aller-ez plus;Alogynan;Antihist-1;Arrest;Benaznyl;Clemastin fumerate syrup;Corto-tavegil;Dexa-tavegil;Fumarsutin;Licasol;Maikohist;Mallermin;Rhinergal tavegil;Tavist 1;Tavist tablets;Tavist-1;Tavist-d;Tavist-syrup.
Therapeutic Function
Antihistaminic
Clinical Use
Antihistamine:
Symptomatic relief of allergy such as hay fever, urticaria
Synthese
Clemastine, 2-[2-[1-(4-chlorophenyl)-1-phenylethoxy]ethyl]-1-methylpyrrolidine (16.1.4), is synthesized by reacting 1-(4-chlorophenyl)-1-phenylethanol (16.1.3) with 2- (2-chlorethyl)-2-methylpyrrolidine using sodium amide as a base. The starting 1-(4-chlorophenyl)-1-phenylethanol (16.1.3) is synthesized either by reacting 4-chlorobenzophenone with methylmagnesium chloride, or by reacting 4-chloroacetophenone with phenylmagnesium bromide.
Arzneimittelwechselwirkung
Potentially hazardous interactions with other drugs
Analgesics: sedative properties increased with opioid analgesics.
Stoffwechsel
Extensively metabolised in the liver mainly by mono- and didemethylation and glucuronide conjugation. The metabolites are mainly excreted in the urine.

CLEMASTINE FUMARATE Upstream-Materialien And Downstream Produkte

CLEMASTINE FUMARATE Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

15686-51-8, CLEMASTINE FUMARATE Verwandte Suche:

Send Inquriy