Welcome to LookChem.com Sign In|Join Free
  • or
Home > Products >  > 

Azelastine
Related Products

Hot Products

Basic Information Post buying leads Suppliers Cas Database
Name

Azelastine

 EINECS 253-720-4
CAS No. 58581-89-8 Density 1.25 g/cm3
PSA 38.13000 LogP 4.23540
Solubility N/A Melting Point N/A
Formula C22H24ClN3O Boiling Point 533.9 °C at 760 mmHg
Molecular Weight 381.905 Flash Point 276.7 °C
Transport Information N/A Appearance white crystal powder
Safety Risk Codes R50/53; R23/25
Molecular Structure Molecular Structure of 58581-89-8 (Azelastine) Hazard Symbols N,T
Synonyms

4-[(4-chlorophenyl)methyl]-2-(1-methylazepan-4-yl)-phthalazin-1-one;

Article Data 7

Azelastine Synthetic route

53242-88-9

4-[(4-chlorophenyl)methyl]-1(2H)-phthalazinone

2-(2-chloroethyl)-1-methylpyrrolidine hydrochloride

A

4-(p-Chlorbenzyl)-2-<2-(N-methylpyrrolidin-2-yl)-ethyl>-1(2H)-phthalazinon

B

58581-89-8

azelastine

Conditions
ConditionsYield
With sodium hydroxide at 70℃; for 1h; Yield given;
53242-76-5

2‐(4-chlorophenylacetyl)benzoic acid

2-Benzoyl-1-(hexahydro-1-methyl-1H-azepin-4-yl)hydrazin-hydrochlorid

58581-89-8

azelastine

Conditions
ConditionsYield
With hydrogenchloride; potassium hydroxide 1.) reflux, 3 h, 2.) methanol, reflux, 2 h; Yield given. Multistep reaction;
1878-66-6

4-chlorophenylacetic Acid

58581-89-8

azelastine

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1: CH3COONa / 3 h / 245 - 250 °C
2: aq. NaOH / 2 h / Heating
3: 1.) 23percent aq. HCl, 2.) KOH / 1.) reflux, 3 h, 2.) methanol, reflux, 2 h
View Scheme
Multi-step reaction with 4 steps
1: CH3COONa / 3 h / 245 - 250 °C
2: aq. NaOH / 2 h / Heating
3: 90 percent / hydrazine sulfate, aq. NaOH / 2 h / Heating
4: aq. NaOH / 1 h / 70 °C
View Scheme
1859-33-2

1-methyl-1,2,3,5,6,7-hexahydroazepin-4-one

58581-89-8

azelastine

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: 2.) NaBH4 / 1.) CH3OH, room temp.
2: 1.) 23percent aq. HCl, 2.) KOH / 1.) reflux, 3 h, 2.) methanol, reflux, 2 h
View Scheme
Multi-step reaction with 3 steps
1.1: potassium hydroxide / water / 1 h / 25 - 35 °C
1.2: 2 h / 0 - 10 °C
2.1: tetrahydrofuran / 1 h / 0 - 10 °C / Reflux
3.1: hydrogenchloride / 2 h / 20 °C / Reflux
3.2: 2 h / Reflux
View Scheme
Multi-step reaction with 3 steps
1.1: potassium hydroxide / water / 1 h / 25 - 35 °C
1.2: 2 h / 0 - 10 °C
2.1: tetrahydrofuran / 1 h / 0 - 10 °C / Reflux
3.1: hydrogenchloride / 2 h / 20 °C / Reflux
3.2: 2 h / Reflux
View Scheme
Multi-step reaction with 3 steps
1.1: potassium hydroxide / water / 1 h / 25 - 35 °C
1.2: 2 h / 0 - 10 °C
2.1: acetonitrile / 1 h / 0 - 10 °C / Reflux
3.1: hydrogenchloride / 2 h / 20 °C / Reflux
3.2: 2 h / Reflux
View Scheme
85-44-9

phthalic anhydride

3-<2-carboxy-phenyl>-pyridine-carboxylic acid-(2)

3-<2-carboxy-phenyl>-pyridine-carboxylic acid-(2)

58581-89-8

azelastine

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1: CH3COONa / 3 h / 245 - 250 °C
2: aq. NaOH / 2 h / Heating
3: 1.) 23percent aq. HCl, 2.) KOH / 1.) reflux, 3 h, 2.) methanol, reflux, 2 h
View Scheme
Multi-step reaction with 4 steps
1: CH3COONa / 3 h / 245 - 250 °C
2: aq. NaOH / 2 h / Heating
3: 90 percent / hydrazine sulfate, aq. NaOH / 2 h / Heating
4: aq. NaOH / 1 h / 70 °C
View Scheme
105279-16-1

(Z)-3-(4-chlorophenyl)methylidenephthalide

58581-89-8

azelastine

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: aq. NaOH / 2 h / Heating
2: 1.) 23percent aq. HCl, 2.) KOH / 1.) reflux, 3 h, 2.) methanol, reflux, 2 h
View Scheme
Multi-step reaction with 3 steps
1: aq. NaOH / 2 h / Heating
2: 90 percent / hydrazine sulfate, aq. NaOH / 2 h / Heating
3: aq. NaOH / 1 h / 70 °C
View Scheme
53242-76-5

2‐(4-chlorophenylacetyl)benzoic acid

58581-89-8

azelastine

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: 90 percent / hydrazine sulfate, aq. NaOH / 2 h / Heating
2: aq. NaOH / 1 h / 70 °C
View Scheme

1H-azepine, 4-hydrazinohexahydro-1-methyl, dihydrochloride

53242-76-5

2‐(4-chlorophenylacetyl)benzoic acid

58581-89-8

azelastine

Conditions
ConditionsYield
Stage #1: 1H-azepine, 4-hydrazinohexahydro-1-methyl, dihydrochloride; 2‐(4-chlorophenylacetyl)benzoic acid With sodium hydroxide In methanol; water for 4h; Heating / reflux;
Stage #2: With hydrogenchloride In methanol; 2,8-dimethylnonan-5-one; water
79307-93-0

azelastine hydrochloride

58581-89-8

azelastine

Conditions
ConditionsYield
With sodium hydroxide In water pH=10; Inert atmosphere;

C14H23N3O(2+)*C4H2O4(2-)

53242-76-5

2‐(4-chlorophenylacetyl)benzoic acid

58581-89-8

azelastine

Conditions
ConditionsYield
Stage #1: C14H23N3O(2+)*C4H2O4(2-) With hydrogenchloride at 20℃; for 2h; Reflux;
Stage #2: 2‐(4-chlorophenylacetyl)benzoic acid for 2h; Reflux;		8.1 g

Azelastine Chemical Properties

Chemical Name: Azelastine  
IUPAC Name: 4-[(4-Chlorophenyl)methyl]-2-(1-methylazepan-4-yl)phthalazin-1-one 
CAS No.: 58581-89-8
Molecular Formula: C22H24ClN3O
Molecular Weight: 381.9 g/mol
Polar Surface Area: 35.91 Å2
Index of Refraction: 1.641
Molar Refractivity: 109.97 cm3
Molar Volume: 304.5 cm3
Surface Tension: 47.4 dyne/cm
Density: 1.25 g/cm3
Flash Point: 276.7 °C
Enthalpy of Vaporization: 81 kJ/mol
Boiling Point: 533.9 °C at 760 mmHg
Vapour Pressure: 1.77E-11 mmHg at 25°C
Following is the structure of Azelastine (CAS NO.58581-89-8):

            
The chemical synonymous of Azelastine (CAS NO.58581-89-8) are 1(2h)-phthalazinone,4-((4-chlorophenyl)methyl)-2-(hexahydro-1-methyl-1h-azepin ; 4-(p-chlorobenzyl)-2-(hexahydro-1-methyl-1h-azepin-4-yl)-1-(2h)-phthalazinon ; AZELASTINE ; 1(2H)-Phthalazinone, 4-[(4-chlorophenyl)methyl]-2-(hexahydro-1-methyl-1H-azepin-4-yl)- ; 4-[(4-chlorophenyl)methyl]-2-(1-methylazepan-4-yl)-phthalazin-1-one ; CAS 790307-93-0 ; 4-[(4-chlorophenyl)methyl]-2-(hexahydro-1-methyl-1H-azepin-4-y1)-1(2H)-phthalazinone .

Azelastine Uses

 Azelastine (CAS NO.58581-89-8) is used for bronchial asthma, nasalallergy treatment.and used as a nasal spray (Astelin or Astepro)for hay fever and as eye drops (Optivar) for allergicconjunctivitis.

Azelastine Toxicity Data With Reference

dog LD50 intravenous 13700ug/kg (13.7mg/kg) BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD

BEHAVIORAL: CHANGES IN MOTOR ACTIVITY (SPECIFIC ASSAY)

GASTROINTESTINAL: NAUSEA OR VOMITING		 Arzneimittel-Forschung. Drug Research. Vol. 31, Pg. 1184, 1981.
dog LD50 oral 51300ug/kg (51.3mg/kg) BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD

BEHAVIORAL: CHANGES IN MOTOR ACTIVITY (SPECIFIC ASSAY)

GASTROINTESTINAL: NAUSEA OR VOMITING		 Arzneimittel-Forschung. Drug Research. Vol. 31, Pg. 1184, 1981.
mouse LD50 intramuscular 59700ug/kg (59.7mg/kg)   Iyakuhin Kenkyu. Study of Medical Supplies. Vol. 17, Pg. 1106, 1986.
mouse LD50 intraperitoneal 42800ug/kg (42.8mg/kg) PERIPHERAL NERVE AND SENSATION: FLACCID PARALYSIS WITHOUT ANESTHESIA (USUALLY NEUROMUSCULAR BLOCKAGE)

BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD

LUNGS, THORAX, OR RESPIRATION: OTHER CHANGES		 Arzneimittel-Forschung. Drug Research. Vol. 31, Pg. 1184, 1981.
mouse LD50 intravenous 25400ug/kg (25.4mg/kg)   Iyakuhin Kenkyu. Study of Medical Supplies. Vol. 17, Pg. 1106, 1986.
mouse LD50 oral 124mg/kg (124mg/kg) PERIPHERAL NERVE AND SENSATION: FLACCID PARALYSIS WITHOUT ANESTHESIA (USUALLY NEUROMUSCULAR BLOCKAGE)

BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD

LUNGS, THORAX, OR RESPIRATION: OTHER CHANGES		 Arzneimittel-Forschung. Drug Research. Vol. 31, Pg. 1184, 1981.
mouse LD50 subcutaneous 54200ug/kg (54.2mg/kg) PERIPHERAL NERVE AND SENSATION: FLACCID PARALYSIS WITHOUT ANESTHESIA (USUALLY NEUROMUSCULAR BLOCKAGE)

LUNGS, THORAX, OR RESPIRATION: OTHER CHANGES

BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD		 Arzneimittel-Forschung. Drug Research. Vol. 31, Pg. 1184, 1981.
rat LD50 intramuscular 115mg/kg (115mg/kg)   Iyakuhin Kenkyu. Study of Medical Supplies. Vol. 17, Pg. 1106, 1986.
rat LD50 intraperitoneal 43200ug/kg (43.2mg/kg) PERIPHERAL NERVE AND SENSATION: FLACCID PARALYSIS WITHOUT ANESTHESIA (USUALLY NEUROMUSCULAR BLOCKAGE)

BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD

LUNGS, THORAX, OR RESPIRATION: OTHER CHANGES		 Arzneimittel-Forschung. Drug Research. Vol. 31, Pg. 1184, 1981.
rat LD50 intravenous 26900ug/kg (26.9mg/kg) PERIPHERAL NERVE AND SENSATION: FLACCID PARALYSIS WITHOUT ANESTHESIA (USUALLY NEUROMUSCULAR BLOCKAGE)

BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD

LUNGS, THORAX, OR RESPIRATION: OTHER CHANGES		 Arzneimittel-Forschung. Drug Research. Vol. 31, Pg. 1184, 1981.
rat LD50 oral 310mg/kg (310mg/kg) PERIPHERAL NERVE AND SENSATION: FLACCID PARALYSIS WITHOUT ANESTHESIA (USUALLY NEUROMUSCULAR BLOCKAGE)

BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD

LUNGS, THORAX, OR RESPIRATION: OTHER CHANGES		 Arzneimittel-Forschung. Drug Research. Vol. 31, Pg. 1184, 1981.
rat LD50 subcutaneous 59600ug/kg (59.6mg/kg) PERIPHERAL NERVE AND SENSATION: FLACCID PARALYSIS WITHOUT ANESTHESIA (USUALLY NEUROMUSCULAR BLOCKAGE)

BEHAVIORAL: CONVULSIONS OR EFFECT ON SEIZURE THRESHOLD

LUNGS, THORAX, OR RESPIRATION: OTHER CHANGES		 Arzneimittel-Forschung. Drug Research. Vol. 31, Pg. 1184, 1981.
 

Azelastine Safety Profile

Poison by ingestion, subcutaneous, intravenous, and intraperitoneal routes. Experimental reproductive effects. When heated to decomposition it emits toxic fumes of NOx and Cl−.

Azelastine Specification

Side effects of Azelastine (CAS NO.58581-89-8) spray vary somewhat depending on the condition being treated. The most common side effects include bitter taste, headache, rhinitis, nose bleed, and somnolence. Adults being treated for vasomotor rhinitis may also experience dysesthesia and sinusitis.

Post a RFQ

Enter 15 to 2000 letters.Word count: 0 letters

Attach files(File Format: Jpeg, Jpg, Gif, Png, PDF, PPT, Zip, Rar,Word or Excel Maximum File Size: 3MB)

1

What can I do for you?
Get Best Price

Get Best Price for 58581-89-8