SPIPERONE Struktur

Spiperon

Bezeichnung:Spiperon

CAS-Nr749-02-0

Englisch Name:SPIPERONE

CBNumberCB5748844

SummenformelC23H26FN3O2

Molgewicht395.47

MOL-Datei749-02-0.mol

Synonyma

Spiperon

Spiperon physikalisch-chemischer Eigenschaften

Schmelzpunkt	190-193.60C
Siedepunkt	630.6±55.0 °C(Predicted)
Dichte	1.1714 (estimate)
storage temp.	Store at RT
Löslichkeit	H2O: slightly soluble0.2mg/mL
pka	pKa 8.31 (Uncertain);9.09 (Uncertain)
Aggregatzustand	solid
Farbe	light yellow
Wasserlöslichkeit	32mg/L(22 ºC)

Sicherheit

Kennzeichnung gefährlicher	Xn
R-Sätze:	22-63
S-Sätze:	36/37
WGK Germany	3
RTECS-Nr.	XX8925000

Gefahreninformationscode (GHS)

SPIPERONE Chemische Eigenschaften,Einsatz,Produktion Methoden

R-Sätze Betriebsanweisung:
R22:Gesundheitsschädlich beim Verschlucken.
R63:Kann das Kind im Mutterleib möglicherweise schädigen.
S-Sätze Betriebsanweisung:
S36/37:Bei der Arbeit geeignete Schutzhandschuhe und Schutzkleidung tragen.
Chemische Eigenschaften
Off-White Solid
Originator
Spiropitan,Eisai,Japan,1969
Verwenden
Spiperone is an antipsychotic.
Verwenden
antibacterial
Definition
ChEBI: An azaspiro compound that is 1,3,8-triazaspiro[4.5]decane which is substituted at positions 1, 4, and 8 by phenyl, oxo, and 4-(p-fluorophenyl)-4-oxobutyl groups, respectively.
Manufacturing Process
A mixture of 4-carbamoyl-4-N-anilinopiperidine and formamide is heated for 12 hours at 170°C. After cooling, the reaction mixture is divided between 100parts water and 900 parts chloroform. The organic layer is separated, dried over MgSO4 filtered and the filtrate is evaporated. The semisolid residue is stirred in ethyl acetate. The undissolved part is filtered off, washed with ethyl acetate, and dried, yielding 1-oxo-4-phenyl-2,4,8- triazaspiro[4.5]decane.
A mixture of 3.2 parts 4-chloro-p-fluoro-butyrophenone, 3.5 parts 1-oxo-4- phenyl-2,4,8-triazaspiro(4,5)decane, 2 parts Na2CO3 and 0.1 part KI in 200 parts hexone is refluxed with stirring for 50 hours. The mixture is cooled to room temperature, 200 parts water are added and the layers are separated. The organic layer is dried over 10 parts MgSO4, filtered and the solvent removed under reduced pressure on the water bath. The residue is treated with 50 parts diisopropylether. The precipitate is filtered on a Buchner filter and recrystallized from 20 parts hexone at room temperature. The solid is filtered off and dried to yield 1-oxo-4-phenyl-8-[3-(4-fluorobenzoyl)-propyl] -2,4,8- triazaspiro(4.5)decane, melting point 190° to 193.6°C, as a light brown amorphous powder.
Trademarks
Spiropitan (Janssen Pharmaceutica, Belgium).
Therapeutic Function
Tranquilizer
Allgemeine Beschreibung
Spiperone is a butyrophenone antipsychotic agent. It induces calcium-dependent chloride secretion in the airway and functions as a potential therapeutic target for cystic fibrosis.
Biologische Aktivität
5-HT 2A serotonin and selective D 2 -like dopamine receptor antagonist (K i values are 0.06, 0.6, 0.08, ~ 350, ~ 3500 nM for D 2 , D 3 , D 4 , D 1 and D 5 receptors respectively). Antipsychotic.
Biochem/physiol Actions
Selective D2 dopamine receptor antagonist; α1B-adrenoceptor antagonist; mixed 5-HT2A/5-HT1 serotonin receptor antagonist; antipsychotic.

SPIPERONE Upstream-Materialien And Downstream Produkte

Spiperon Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

749-02-0, SPIPERONE Verwandte Suche:

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