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DROPERIDOL

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DROPERIDOL Basic information

Product Name:
DROPERIDOL
Synonyms:
  • DROPERIDOL
  • 1-(1-[4-FLUOROBENZOYLPROPYL]-1,2,3,6-TETRAHYDRO-4-PYRIDYL)-2-BENZIMIDAZOLINONE
  • 1-[1-(P-FLUOROBENZOYLPROPYL)-1,2,3,6-TETRAHYDRO-4-PYRIDYL]-2-BENZIMIDAZOLINONE
  • 1-(1-(3-(p-fluorobenzoyl)propyl)-1,2,3,6-tetrahydro-4-pyridyl)-2-benzimidazo
  • 1-(1-(3-(p-Fluorobenzoyl)propyl)-1,2,3,6-tetrahydro-4-pyridyl)-2-benzimidazolinone
  • 1-(1-(4-(4-fluorophenyl)-4-oxobutyl)-1,2,3,6-tetrahydro-2h-benzimidazol-2-on
  • 1-(1-(4-(p-fluorophenyl)-4-oxobutyl)-1,2,3,6-tetrahydro-4-pyridyl)-2-benzimi
  • 1-(1-(4-(p-Fluorophenyl)-4-oxobutyl)-1,2,3,6-tetrahydro-4-pyridyl)-2-benzimidazolinone
CAS:
548-73-2
MF:
C22H22FN3O2
MW:
379.43
EINECS:
208-957-8
Product Categories:
  • PEPCID
  • Other APIs
  • Heterocyclic Compounds
  • Heterocycles
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
Mol File:
548-73-2.mol
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DROPERIDOL Chemical Properties

Melting point:
148-149°C
Density 
1.2154 (estimate)
storage temp. 
2-8°C
solubility 
Practically insoluble in water, freely soluble in dimethylformamide and in methylene chloride, sparingly soluble in ethanol (96 per cent).
pka
7.64(at 25℃)
form 
neat
Water Solubility 
4.1mg/L(30 ºC)
CAS DataBase Reference
548-73-2(CAS DataBase Reference)
EPA Substance Registry System
2H-Benzimidazol-2-one, 1-[1-[4-(4-fluorophenyl)-4-oxobutyl]-1,2,3,6-tetrahydro-4-pyridinyl]-1,3-dihydro- (548-73-2)
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Safety Information

Hazard Codes 
Xn
Risk Statements 
22
Safety Statements 
36
RIDADR 
3249
WGK Germany 
3
RTECS 
DE2100000
HazardClass 
6.1(b)
PackingGroup 
III
HS Code 
2933995800
Toxicity
LD50 oral in rat: 750mg/kg

MSDS

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DROPERIDOL Usage And Synthesis

Chemical Properties

Pale Yellow Solid

Originator

Dehydrobenzperidol,Janssen,W. Germany,1963

Uses

A D1, D2 dopamine receptor antagonist; butyrophenone antipsychotic and anti-emetic.

Uses

H2 antihistamine

Uses

A D1DR and D2DR inhibitor.

Definition

ChEBI: An organofluorine compound that is haloperidol in which the hydroxy group has been eliminated with the introduction of a double bond in the piperidine ring, and the 4-chlorophenyl group has been replaced by a benzimidazol-2-on-1-yl group. It is used in the management of chemotherapy-induced nausea and vomiting, and in conjunction with an opioid analgesic such as fentanyl to maintain the patient in a calm state of neuroleptanalgesia with indifference to surroundings but still able to cooperate with the surgeo .

Manufacturing Process

A mixture of 10 parts of γ-chloro-4-fluorobutyrophenone, 5.5 parts of 1- (1,2,3,6-tetrahydro-4-pyridyl)-2-benzimidazolinone, 4 parts of sodium carbonate, and 0.1 part of potassium iodide in 176 parts of 4-methyl-2- pentanone is stirred and refluxed for 64 hours. The cooled reaction mixture is filtered and the solvent is evaporated from the filtrate to leave an oily residue which is dissolved in toluene. The toluene solution is filtered and the solvent is evaporated. The resultant residue is recrystallized from a mixture of 32 parts of ethyl acetate and 32 parts of diisopropyl ether to give 1-[1-[(4-fluorobenzoyl)propyl]-1,2,3,6-tetrahydro-4-pyridyl]-2-benzimidazolinone hydrate melting at about 145°-146.5°C.

brand name

Inapsine (Akorn);Dehydrobenzperidol;Diaperidol;Inopsin.

Therapeutic Function

Tranquilizer

General Description

Droperidol, 1-{1-[3-(p-fluorobenzoyl)propyl]-1,2, 3,6-tetrahydro-4-pyridyl}-2-benzimidazolinone(Inapsine), may be used alone as a preanestheticneuroleptic or as an antiemetic. Because of its very shortactingand highly sedating properties, its most frequent useis in combination (Innovar) with the narcotic agent fentanyl(Sublimaze) preanesthetically.

General Description

Droperidol, 1-1-[3-(p-fluorobenzoyl)propyl]-1,2,[3,6-tetrahydro-4-pyridyl]-2-benzimidazolinone(Inapsine). Centrally acting acetylcholinesteraseinhibitors may increase the risk of antipsychotic-relatedEPS. CNS depressants may produce additive sedativeeffects (benzodiazepines, barbiturates, antipsychotics,ethanol, opiates, and other sedative medications).Droperidol in combination with certain forms of inhalationanesthetics may produce peripheral vasodilatation and hypotension.Metoclopramide may increase the risk of EPSproduced by droperidol.

DROPERIDOLSupplier

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