Bunazosin hydrochloride Chemical Properties

Melting point:

280-282°

storage temp. 

Sealed in dry,Room Temperature

solubility 

DMSO (Slightly, Heated), Methanol (Slightly, Heated)

form 

Solid

color 

White to Off-White

Stability:

Hygroscopic

Safety Information

Toxicity

LD50 oral in rat: 980mg/kg

Bunazosin hydrochloride Usage And Synthesis

Description

Bunazosin hydrochloride is a selective αl-adrenergic antagonist related to prazosin and useful in the treatment of hypertension.

Originator

Eisai (Japan)

Uses

Bunazosin Hydrochloride is an α-1 adrenergic receptor antagonist that acts as an anti-cancer and anti-glaucoma drug.

Definition

ChEBI: Bunazosin hydrochloride is a member of quinazolines.

Manufacturing Process

17.0 g of 2-chloro-4-amino-6,7-dimethoxyquinazoline and 18.2 g of Nformylhomopiperazine are added to 170 ml of butanol and the whole is refluxed with stirring for 3 h. After completion of the reaction, the mixture is cooled, and the crystals thus precipitated are filtered out, washed with a small quantity of ethanol and air-dried. 25.0 g of crude 2-homopiperazino-4-amino- 6,7-dimethoxyquinazoline are obtained.
A solution of 2-homopiperazino-4-amino-6,7-dimethoxyquinazoline in 60 ml of acetone is added dropwise to a solution of 2-butylcarboxylic acid chloride in acetone under stirring and ice-cooling. After completion of the addition, the stirring is continued for additional 1 h to complete the reaction. The crystals thus precipitated are filtered out and the 1-(4-amino-6,7-dimethoxy-2- quinazolinyl)hexahydro-4-(1-oxobutyl)-1H-1,4-diazepine, melting point 280- 282°C (recrystallized from a mixture of methanol-ethanol) is obtained.

brand name

DETANTOL

Therapeutic Function

Antihypertensive

Bunazosin hydrochloride(52712-76-2)Related Product Information

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