ChemicalBook--->CAS DataBase List--->52712-76-2

52712-76-2

52712-76-2 Structure

52712-76-2 Structure
IdentificationBack Directory
[Name]

Bunazosin hydrochloride
[CAS]

52712-76-2
[Synonyms]

E-643
E 1015
E-1015
Detantol
Detantol-R
Bunzaosin Hcl
Bunazosin Hcl
Bunazosin, DETANTO
BUNAZOSIN HYDROCHLORIDE
Bunazosin hydrochloride USP/EP/BP
1-[4-(4-amino-6,7-dimethoxy-2-quinazolinyl)-1,4-diazepan-1-yl]-1-butanone
1-[4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-1,4-diazepan-1-yl]butan-1-one hydrochloride
1-(4-Amino-6,7-dimethoxyquinazolin-2-y1)-4-butyrylhexahydro-lH-1,4-diazepine hydrochloride
[Molecular Formula]

C19H28ClN5O3
[MDL Number]

MFCD00941411
[MOL File]

52712-76-2.mol
[Molecular Weight]

409.91
Chemical PropertiesBack Directory
[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
Raw materials And Preparation ProductsBack Directory
[Raw materials]

Anisole-->Benzonitrile-->Butyryl chloride-->Quinazoline-->1-Formylhomopiperazine-->Bunazosin-->2-Chloro-4-amino-6,7-dimethoxyquinazoline
Hazard InformationBack Directory
[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
Safety DataBack Directory
[Toxicity]

LD50 oral in rat: 980mg/kg
Spectrum DetailBack Directory
[Spectrum Detail]

Bunazosin hydrochloride(52712-76-2)1HNMR
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