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Brimonidine Manufacturer/High quality/Best price/In stock
Cas No: 59803-98-4
USD $ 3.0-3.0 / Kilogram 1 Kilogram 1-100 Metric Ton/Month Dayang Chem (Hangzhou) Co.,Ltd. Contact Supplier
High quality 5-Bromo-6-(Imidazolin-2-Ylamino)Quinoxaline supplier in China
Cas No: 59803-98-4
No Data 1 Metric Ton 30 Metric Ton/Month Simagchem Corporation Contact Supplier
brimonidine manufacturer/supplier
Cas No: 59803-98-4
No Data 1 Gram 1000 Metric Ton/Month Hangzhou JINLAN Pharm-Drugs Technology Co., Ltd Contact Supplier
Brimonidine
Cas No: 59803-98-4
No Data No Data No Data Chemwill Asia Co., Ltd. Contact Supplier
High Quality 99% 5-Bromo-6-(Imidazolin-2-Ylamino)Quinoxaline 59803-98-4 GMP manufacturer
Cas No: 59803-98-4
USD $ 0.1-0.1 / Gram 1 Gram 100 Metric Ton/Year Xi'an Xszo Chem Co., Ltd. Contact Supplier
Factory Supply 5-Bromo-6-(Imidazolin-2-Ylamino)Quinoxaline
Cas No: 59803-98-4
No Data 1 1 Ality Chemical Corporation Contact Supplier
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No Data 10 Milligram Amadis Chemical Co., Ltd. Contact Supplier
Brimonidine CAS 59803-98-4
Cas No: 59803-98-4
USD $ 10.0-10.0 / Kilogram 1 Kilogram 1 Metric Ton/Month Wuhan Fortuna Chemical Co.,Ltd Contact Supplier
Brimonidine
Cas No: 59803-98-4
USD $ 1.0-1.0 / Kilogram 1 Kilogram 2000 Metric Ton/Year Henan Sinotech Import&Export Corporation Contact Supplier
New production CAS 59803-98-4 with best quality
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USD $ 139.0-210.0 / Kilogram 1 Kilogram 1000 Kilogram/Day Zhuozhou Wenxi import and Export Co., Ltd Contact Supplier

59803-98-4 Usage

Description

Launched in the US for open-angle glaucoma and ocular hypertension, brimonidine is a relatively selective and potent α2a,-adrenergic agonist with low affinity for the imidazoline l1 receptor. Topical application reduces intraocular pressure. This bypasses any central hypotensive effects at the l1 receptor (which can also give rise to a decrease in blood pressure and heart rate) if given systemically, since topical application results in low plasma levels concomitant with rapid systemic elimination. Brimonidine can be prepared in a four-step sequence from 4-nitrophenylenediamine.

Uses

coronary vasodilator calcium ion influx inhibitor

Biological Activity

Full α 2 adrenergic agonist. Centrally active following systemic administration in vivo . Also available as part of the α 2 -Adrenoceptor Tocriset? and Mixed Adrenergic Tocriset? .

Hazard

A poison by ingestion.

Uses

a2-Adrenoceptor agonist. Antiglaucoma

Therapeutic Function

Antiglaucoma

Veterinary Drugs and Treatments

Brimonidine is an alpha-adrenergic receptor agonist. It has a peak ocular hypotensive effect occurring at two hours post-dosing. Fluorophotometric studies in animals and humans suggest that brimonidine tartrate has a dual mechanism of action by reducing aqueous humor production and by and increasing uveoscleral outflow. After ocular administration of either a 0.1% or 0.2% solution, plasma concentrations peaked within 0.5 to 2.5 hours and declined with a systemic half-life of approximately 2 hours. In humans, systemic metabolism of brimonidine is extensive. It is metabolized primarily by the liver. Urinary excretion is the major route of elimination of the drug and its metabolites. Approximately 87% of an orally-administered radioactive dose was eliminated within 120 hours, with 74% found in the urine.

Originator

Allergan (USA)

Chemical Properties

Yellow Solid

Uses

α2-Adrenoceptor agonist. Antiglaucoma.

Manufacturing Process

6-Aminoquinoxaline (2.08 g, 14.4 mmol) was dissolved in 11.5 ml glacial acetic acid. The solution was cooled in water while a solution of bromine (0.74 ml, 2.3 g, 14.4 mmol) in 1.5 ml glacial acetic acid was added slowly over 15 min. After stirring for an additional 30 min. the orange red solid formed was filtered off and washed thoroughly with dry ether. The solid was dried in vacuo overnight to yield 4.44 g crude product (a yield of 100%). The compound, 6- amino-5-bromoquinoxaline hydrobromide, had no definite melting point. A phase change (from fine powder to red crystals) was noticed at about 220°C. Decomposition was observed at about 245°C. It was used directly for the next step. The crude 6-amino-5-bromoquinoxaline from above was dissolved in water and saturated sodium bisulfite solution was added until the resulting solution tested negative with starch-iodide paper. The solution was then basified with 2 N sodium hydroxide and extracted thoroughly with ethyl acetate. The organic extract was dried over magnesium sulfate and concentrated under reduced pressure to give the free base. The crude product was recrystallized from boiling benzene to give yellow crystals, m.p. 155°-156°C. Using various analytical procedures, the yellow crystals were determined to be 6-amino-5- bromoquinoxaline. The yield was 82%. The crude hydrobromide product previously noted (4.27 g, 14.0 mmol) was dissolved in 60 ml of water and thiophosgene (1.28 ml, 16.8 mmol) was added in small portions with vigorous stirring. After 2 hours, the red color of the solution was discharged. The solid formed was filtered off and washed thoroughly with water. After drying in vacuo at 25°C 3.38 g (a yield of 90%) of brick red crystals was obtained, m.p. 157°-158°C. A portion of this material was further purified by column chromatography to give white crystals, m.p. 157°-158°C. Using various analytical procedures, these crystals were determined to be 5-bromo-6-isothiocyanatoquinoxaline. A solution of the isothiocyanate (3.25 g, 12.2 mmol) in 145 ml benzene was added to a solution of ethylenediamine (5.43 g, 90.0 mmol) in 18 ml benzene at 25°C over 2 hours. After stirring for a further 30 min., the supernatant was poured off. The oil which remained was washed by swirling with dry ether three times and used directly for the next step. A portion of this product was further purified by column chromatography (SiO2, CHCl3) for characterization. A white solid was decomposed at 175°C. This white solid was determined to be 5-bromo-6-(N-2-(aminoethyl)thioureido)quinoxaline. The crude product from above was dissolved in 100 ml dry methanol and the brown solution was refluxed for 19 hours until hydrogen sulfide gas was no longer evolved. The mixture was cooled to room temperature and concentrated to about 50 ml. The yellow solid was filtered off and dried in vacuo; weight 2.52 g (a yield of 70%), m.p. 242°-244°C. As the crude product was insoluble in most common organic solvents, initial purification was achieved by an acid-base extraction procedure. 23 g of the crude product was dissolved in 100 ml 0.5 N hydrochloric acid. The turbid yellow solution was filtered to give a clear orange yellow solution which was extracted twice with ethyl acetate (2x10 ml). The aqueous phase was cooled to 0°C and basified with 6 N sodium hydroxide, keeping the temperature of the solution below 15°C at all times. The yellow solid which precipitated was filtered off and washed thoroughly with water until the washings were neutral to pH paper. The solid was dried overnight in vacuo to give 1.97 g yellow solid, m.p. 249°-250°C. The recovery was about 88%. Further purification was achieved by recrystallization as described below. The partially purified product from above was dissolved in N,N-dimethylformamide (about 17 ml/g) at 100°C with vigorous stirring. The solution was filtered hot and set aside to cool overnight. The bright yellow crystals were collected by filtration, m.p. 252°-253°C. Recovery was from 65-77%. Using various analytical procedures the bright yellow solid was determined to be 5-bromo-6- (2-imidazolin-2-ylamino)quinoxaline.

Brand name

Alphagan (Allergan).
InChI:InChI=1/C11H10BrN5/c12-9-7(17-11-15-5-6-16-11)1-2-8-10(9)14-4-3-13-8/h1-4H,5-6H2,(H2,15,16,17)

59803-98-4 Well-known Company Product Price

Brand (Code)Product description CAS number Packaging Price Detail
TCI America (B4132)  Brimonidine  >98.0%(HPLC)(T) 59803-98-4 200mg 750.00CNY Detail
TCI America (B4132)  Brimonidine  >98.0%(HPLC)(T) 59803-98-4 1g 2,450.00CNY Detail
Sigma (U104)  UK 14,304   59803-98-4 U104-5MG 766.35CNY Detail
Sigma (U104)  UK 14,304   59803-98-4 U104-25MG 2,806.83CNY Detail
Sigma (U104)  UK 14,304   59803-98-4 U104-100MG 9,003.15CNY Detail

59803-98-4SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 12, 2017

Revision Date: Aug 12, 2017

1.Identification

1.1 GHS Product identifier

Product name brimonidine

1.2 Other means of identification

Product number -
Other names Bromoxidine

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:59803-98-4 SDS

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